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HK1189589A - Nampt and rock inhibitors - Google Patents

Nampt and rock inhibitors Download PDF

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Publication number
HK1189589A
HK1189589A HK14102695.8A HK14102695A HK1189589A HK 1189589 A HK1189589 A HK 1189589A HK 14102695 A HK14102695 A HK 14102695A HK 1189589 A HK1189589 A HK 1189589A
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HK
Hong Kong
Prior art keywords
dihydro
phenyl
isoindole
carboxylic acid
acid amide
Prior art date
Application number
HK14102695.8A
Other languages
Chinese (zh)
Inventor
Michael L. Curtin
Bryan K. Sorensen
Howard R. Heyman
Richard F. Clark
Kevin R. Woller
Omar J. Shah
Michael Michaelides
Chris Tse
Anil Vasudevan
Helmut Mack
Todd M. Hansen
Ramzi Sweis
Marina A. Pliushchev
Original Assignee
Abbvie Inc.
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Filing date
Publication date
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Publication of HK1189589A publication Critical patent/HK1189589A/en

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Description

NAMPT and ROCK inhibitors
Information of related applications
The present application claims the benefit of U.S. provisional patent application serial No.61/413,722 (applied on 11/15/2010), U.S. provisional patent application serial No.61/474,015 (applied on 11/4/2011), and U.S. provisional patent application serial No.61/525,405 (applied on 19/8/2011), the contents of each of which are incorporated herein by reference.
Technical Field
The present invention relates to compounds that inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. The invention also relates to compounds that inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.
Background
NAD + (nicotinamide adenine dinucleotide) is a coenzyme that plays a key role in many major physiological processes (Ziegkel, M.Eur.J.biochem.267, 1550-. Some signaling pathways require NAD, and such signaling pathways include, among others: multiple ADP-ribosylation in DNA repair, single ADP-ribosylation in immune system and G protein coupling signals, and sirtuins also require NAD for their deacetylase activity (Garten, a. et al Trends in Endocrinology and Metabolism, 20, 130-.
NAMPT (also known as pre-B cell clone enhancing factor (PBEF) and visfatin) is an enzyme that catalyzes the phosphoribosylation of nicotinamide and is the rate-limiting enzyme in one of two pathways for rescuing NAD.
There is increasing evidence that NAMPT inhibitors have potential as anti-cancer agents. Cancer cells have a higher basal cycle of NAD compared to normal cells and show a higher energy requirement. In addition, increased NAMPT expression in colorectal cancer has been reported (Van Beijnum, J.R. et al int.J.cancer 101, 118-. It has been demonstrated in xenograft models that small molecule inhibitors of NAMPT cause depletion of intracellular NAD + levels and ultimately induce tumor cell death (Hansen, CM et al Anticancer Res.20, 42111-.
NAMPT inhibitors also have potential as therapeutics for inflammation and metabolic disorders (gali, m. et al Cancer res.70, 8-11, 2010). For example, NAMPT is the major enzyme in T and B lymphocytes. Selective inhibition of NAMPT leads to NAD + depletion in thymus-dependent cells, blocking the expansion of processes with autoimmune diseases, but sparing cell types expressing other NAD + formation pathways. Small molecule NAMPT inhibitors (FK866) have been shown to selectively block proliferation, induce apoptosis of activated T cells, and to be effective in animal models of arthritis (collagen-induced arthritis) (Busso, n. et al Plos One 3, e2267, 2008). FK866 improves the manifestation of Experimental Autoimmune Encephalomyelitis (EAE), a model of T cell-mediated autoimmune disorders (Bruzzone, S et al Plos One 4, e7897, 2009). NaMPT activity increases NF-kB transcriptional activity in human vascular endothelial cells, leading to activation of MMP-2 and MMP-9, suggesting a role for NaMPT inhibitors in preventing inflammation-mediated complications of obesity and type II Diabetes (Adya, r. et al Diabetes Care, 31, 758-.
Rho kinases (ROCKs), the first Rho effector described, are serine/threonine kinases important for essential processes of cell migration, cell proliferation and cell survival. Aberrant activation of the Rho/ROCK pathway has been observed in a variety of disorders. Compounds having ROCK inhibition, due to their anti-vasospastic activity, have potentially beneficial therapeutic effects on disease states, examples of which include cardiovascular diseases such as hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension and atherosclerosis. This muscle relaxation property is also beneficial in the treatment of asthma, male erectile dysfunction, female sexual dysfunction and overactive bladder. Injury to the brain and spinal cord of adult vertebrates activates ROCKs, thereby inhibiting axon growth and sprouting. After acute neuronal injury in mammals (spinal cord injury, traumatic brain injury), inhibition of ROCKs induces new axonal growth, which re-crosses lesions in the CNS, promotes regeneration and enhances functional recovery. Inhibition of the Rho/ROCK pathway has also proven effective in other animal models of neurodegenerative (e.g., stroke, inflammatory and demyelinating diseases, alzheimer's disease) and pain treatment. Rho/ROCK pathway inhibitors therefore have the potential to prevent neurodegeneration and stimulate neuronal regeneration in various neurological disorders (including spinal cord injury, alzheimer's disease, stroke, multiple sclerosis, amyotrophic lateral sclerosis) and to treat pain. ROCK inhibitors have been shown to have anti-inflammatory properties. Thus, the compounds of the present invention may be useful in the treatment of neuroinflammatory disorders such as stroke, multiple sclerosis, alzheimer's disease, huntington's chorea, parkinson's disease, amyotrophic lateral sclerosis and inflammatory pain, as well as other diseases such as rheumatoid arthritis, osteoarthritis, asthma, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus and inflammatory bowel disease. Since ROCK inhibitors reduce cell proliferation and cell migration, they can be used to treat cancer and tumor metastasis. Furthermore, there is evidence that ROCK inhibitors inhibit cytoskeletal rearrangement caused by viral entry, and thus they also have potential therapeutic value in antiviral and antibacterial applications. ROCK inhibitors are also useful in the treatment of insulin resistance and diabetes. Further, ROCK inhibitors have been shown to improve the progression of cystic fibrosis (Abstract S02.3, 8th world consistency on Inflammation, Copenhagen, Denmark, June 16-20, 2007).
Furthermore, Rho-associated coiled-coil-forming protein kinases (ROCK) -1 and-2 have been shown to increase phosphorylation of Myosin Light Chain (MLC) by inhibiting MLC phosphatase and phosphorylating MLC. This results in modulation of actin-myosin contractile action. Recent reports indicate that inhibition of ROCK can disrupt chemotaxis of inflammatory cells and inhibit smooth muscle contraction in models of pulmonary inflammation associated with asthma. Thus, inhibitors of the Rho/ROCK pathway are useful in the treatment of asthma.
Summary of the invention
Accordingly, one embodiment of the present invention is directed to compounds useful as inhibitors of NAMPT or ROCK, having formula (Ic), and pharmaceutically acceptable salts thereof
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R2Is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R2Is optionally substituted with one, two, three or four groups independently selected from: r 4，OR4，SR4，S(O)R4，SO2R4，C(O)R4，CO(O)R4，OC(O)R4，OC(O)OR4，NHC(O)R4，NR4C(O)R4，NHS(O)2R4，NR4S(O)2R4，NHC(O)OR4，NR4C(O)OR4，NHC(O)NH2，NHC(O)NHR4，NHC(O)N(R4)2，NR4C(O)NHR4，NR4C(O)N(R4)2，C(O)NH2，C(O)NHR4，C(O)N(R4)2，C(O)NHOH，C(O)NHOR4，C(O)NHSO2R4，C(O)NR4SO2R4，SO2NH2，SO2NHR4，SO2N(R4)2，C(O)H，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each R2The phenyl group of (a) is additionally optionally substituted with one F; wherein each R2The heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R3independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R4independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Is optionally substituted with one, two, three or four groups independently selected from: r7，OR7，SR7，S(O)R7，SO2R7，C(O)R7，OC(O)R7，OC(O)OR7，NH2，NHR7，NHC(O)R7，NR7C(O)R7，NHS(O)2R7，NR7S(O)2R7，NHC(O)OR7，NR7C(O)OR7，NHC(O)NH2，NHC(O)NHR7，NHC(O)N(R7)2，NR7C(O)NHR7，NR7C(O)N(R7)2，C(O)NH2，C(O)NHR7，C(O)N(R7)2，C(O)NHOH，C(O)NHOR7，C(O)NHSO2R7，C(O)NR7SO2R7，SO2NH2，SO2NHR7，SO2N(R7)2，C(O)H，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R4The aryl and heterocyclyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r8，OR8，SR8，S(O)R8，SO2R8，C(O)R8，CO(O)R8，OC(O)R8，OC(O)OR8，NH2，NHR8，NHC(O)R8，NR8C(O)R8，NHS(O)2R8，NR8S(O)2R8，NHC(O)OR8，NR8C(O)OR8，NHC(O)NH2，NHC(O)NHR8，NHC(O)N(R8)2，NR8C(O)NHR8，NR8C(O)N(R8)2，C(O)NH2，C(O)NHR8，C(O)N(R8)2，C(O)NHOH，C(O)NHOR8，C(O)NHSO2R8，C(O)NR8SO2R8，SO2NH2，SO2NHR8，SO2N(R8)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5at each time of dischargeWhen present, is independently selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R7independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R7Is optionally substituted with one, two, three or four groups independently selected from: r11，OR11,SR11，S(O)R11，SO2R11，NHR11，N(R11)2，C(O)R11，C(O)NH2，C(O)NHR11，C(O)N(R11)2，NHC(O)R11，NR11C(O)R11，NHSO2R11，NHC(O)OR11，SO2NH2，SO2NHR11，SO2N(R11)2，NHC(O)NH2，NHC(O)NHR11，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R8independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12，SR12，S(O)R12，SO2R12，NHR12，N(R12)2，C(O)R12，C(O)NH2，C(O)NHR12，C(O)N(R12)2，NHC(O)R12，NR12C(O)R12，NHSO2R12，NHC(O)OR12，SO2NH2，SO2NHR12，SO2N(R12)2，NHC(O)NH2，NHC(O)NHR12，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R11independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R12independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R12The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more alkoxy groups;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R 13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkylAlkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r 16，OR16OH, F, Cl, Br or I; wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
R15independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted with one, two, three or four alkoxy groups;
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
Another embodiment relates to compounds having the formula (Vc) and pharmaceutically acceptable salts thereof
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ] ]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally one, two, three or four independently selected fromThe following groups: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl, wherein R is15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
Provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
Another embodiment relates to compounds having formula (Ic) or formula (Vc) and pharmaceutically acceptable salts thereof; wherein X1、X2And X3Is CH, or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1。
Another embodiment relates to compounds having formula (Ic) or formula (Vc) and pharmaceutically acceptable salts thereof; wherein X1And X3Is CH; x2Is N; or X2Is CH; x1And X3Is N; x2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N.
Another embodiment is directed to compounds having formula (Ic) and pharmaceutically acceptable salts thereof, wherein R2Is at para position by R5Substituted phenyl; r5Is phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, pyrrolo [1, 2-d][1，2，4]Triazin-1 (2H) -one or isoindolin-1-one.
Another embodiment relates to compounds of formula (Ic) which are:
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (furo [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (thieno [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dihydro-1, 4-benzodioxin-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ 3-fluoro-5- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-acetylphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (2, 3-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (6-aminohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-benzodioxol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dihydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-propoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-2-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methyl-1H-indazol-5-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (2, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 5- ({4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } amino) -1H-indazole-3-carboxylate;
n- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (5-chloropyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 3-dihydro-1, 4-benzodioxin-6-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-fluorobenzoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methoxy-1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-propoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (dimethylamino) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoro-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1, 3-benzodioxol-5-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- {4- [ (2-phenoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-hydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (3-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({1- [ (3S) -tetrahydrofuran-3-yl ] -1H-pyrazol-4-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 4-dioxa-8-azaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylthio) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (trifluoromethyl) thio ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-fluorophenyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (1H-imidazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (hydroxymethyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-benzodioxol-5-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-isopropyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiomorpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzylpiperidin-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-acetylamino-2-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (3, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [3- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-imidazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1- (3-cyanophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (2-hydroxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyanomethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclohexylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 4-dihydroisoquinolin-2 (1H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1H-indol-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (phenylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (diethylamino) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-hydroxy-2-phenylethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-aminophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } piperidin-4-yl) carbamate;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ 3-chloro-5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (cyclohexylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-chlorobenzyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (diethylcarbamoyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (2-hydroxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-6-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5, 6-dihydro [1, 2, 4] triazolo [4, 3-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-fluoropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylmethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3, 4, 9-tetrahydro-2H- β -carbolin-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tert-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [4- (trifluoromethyl) phenyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-difluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-benzylpyrrolidin-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-carbamoylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopropylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (methylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dioxolan-2-ylmethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (4-fluorophenyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-hydroxy-2-methylprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-phenyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({2- [4- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (sec-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (ethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isobutyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4-carbamoylphenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (trifluoromethyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 6-dimethylmorpholin-4-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (prop-2-yn-1-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyanoethyl) (cyclopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (isopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -N-isopropyl- β -alanine;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5, 6-dimethoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-chlorophenoxy) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenyl-1, 3-thiazol-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid;
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (aminomethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (2-hydroxy-2-methylpropanoyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetylamino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (N, N-dimethylglycyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methoxyacetyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methylsulfonyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4, 4, 4-trifluorobutanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-methylpentanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (benzyloxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ N- (2-furoyl) glycyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-thienyl) butyryl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-oxo-4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (N-benzoylglycyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenoxybutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (propionylamino) phenyl ] -amide;
n- [4- (pentanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (heptanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (pent-4-enoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-methylpiperazin-1-yl) propionyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylate;
2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyclopentylethyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester;
n- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-methyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1E) -5-phenylpent-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxyethyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (1-propyl-1H-pyrazol-4-yl) pyridin-3-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-phenylpentyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [ 2-fluoro-4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 2-fluoro-4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (isopropylsulfonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-benzoylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (isopropylsulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (benzenesulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (benzoylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (butyrylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperazine-1-carboxylic acid tert-butyl ester;
N- [4- (4-propionylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopropylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-butanoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-isobutyryl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-benzoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [2- (3-methylbutyl) -2, 3-dihydro-1H-isoindol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexyloxy) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (4-chlorophenoxy) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (piperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n, N' -hexane-1, 6-diylbis (1, 3-dihydro-2H-isoindole-2-carboxylic acid amide);
n- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
Ethyl 6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] hexanoate;
n-hexyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n-octyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (1-methyl-1H-pyrazol-4-yl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (methylamino) -6-oxohexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 6-oxo-6- [ (3-phenylpropyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-methylbutyl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (5- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-phenylpropyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-phenylpropyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4, 5, 6, 7, 8-hexahydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (8-fluoro-4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl]-1，3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (morpholin-4-ylmethyl) -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-4, 5-dihydro-3H-2, 3-benzodiazepine-1-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (1-methylpiperidin-4-yl) oxy ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3R) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3S) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (azetidin-1-ylmethyl) -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperidine-1-carboxylic acid tert-butyl ester;
n- [4- (5-propyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (piperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [5- (3-methylbutyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-benzyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-chloropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-oxopyrrolidin-1-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxy-2, 3-dihydro-1H-inden-1-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-hydroxycyclopropyl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] -1H-benzimidazol-2-yl } piperazine-1-carboxylic acid tert-butyl ester;
n- [2- (piperazin-1-yl) -1H-benzoimidazol-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-benzoylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (tetrahydrofuran-3-yl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- (4- { [ (3-phenylpropyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- {4- [1- (4-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (tetrahydrofuran-3-ylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2S) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2R) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-phenylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-methoxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (2-hydroxyethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-3-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-4-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- (2-methoxyethyl) -N2- {4- [ (propylamino) carbonyl group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- (4-cyanophenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (trifluoromethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (tetrahydrofuran-3-ylmethyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-pyridin-2-ylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (1, 2-dihydroxyethyl) -N- {4- [ (propylamino) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-butyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and
n- [2- (4-acetylpiperazin-1-yl) -1H-benzimidazol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (5-oxo-D-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (ethoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-chlorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [3- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-furoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-thienylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrrol-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2, 5-dimethyl-1H-pyrrol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 3-thiazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3, 5-dimethyl-1, 2-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (pyridin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isonicotinoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridazin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrimidin-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- (4- {1- [3- (piperidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [6- (benzoylamino) hexyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (benzoylamino) methyl ] benzyl } carbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-L-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-D-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (1-acetylpiperidin-4-yl) carbonyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-acetamidobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (methylsulfonyl) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-butyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isobutyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-methylbutyryl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 3, 3-trifluoropropionyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (methoxyacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopentylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclohexylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (4-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [3- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 4-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 5-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (3, 4-dimethoxyphenyl) acetyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrrol-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrazol-5-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (pyridin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isonicotinyl piperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridazin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrazin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrimidin-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (N, N-dimethyl- β -alanyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-acetylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (phenylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1, 3-thiazol-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (morpholin-4-ylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxo-2, 3-dihydro-1H-isoindol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1- (2-phenylethyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- [2- (dimethylamino) ethyl group]-N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (morpholin-4-ylcarbonyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { benzyl [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (isobutoxycarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 4- { [ (5-cyano-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoate;
n- (4- { (E) - [ (benzyloxy) imino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (3-aminopyrrolidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-methylbutyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-phenylpropyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- [4- ({ benzyl [3- (morpholin-4-yl) propyl ] amino } methyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-methyl-1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-methoxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (aminomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4- (methylthio) but-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3S) -1-hydroxy-3-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3R) -1, 3-dihydroxybutan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxyhex-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypentan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2R) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-cyclohexyl-3-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ (2R) -1-hydroxy-3- [ (4-methylbenzyl) thio ] propan-2-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1S) -1- (4-tert-butylphenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methoxy-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- [6- (benzoylamino) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (2-methoxyethoxy) acetyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] pyrazin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6-acetamidohexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (1E) -3- [ benzyl (methyl) amino ] prop-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-phenoxypiperidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-phenoxyazetidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ benzyl (methyl) amino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-hydroxy-2-methylpropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbutyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (tetrahydrofuran-3-ylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [2- (2-oxopyrrolidin-1-yl) ethyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1-benzylpiperidin-4-yl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-phenylpropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (morpholin-4-yl) benzyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxypropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {5- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {1 '- [ (2-methoxyethoxy) acetyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [4- (methylsulfonyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (ethoxyacetyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (cyclopentylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (3-cyanobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-cyanobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [3- (dimethylamino) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [4- (dimethylamino) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [3- (trifluoromethyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [4- (trifluoromethyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [3- (trifluoromethoxy) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 3-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 4-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 5-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (phenylacetyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (3-fluorophenyl) acetyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (morpholin-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [6- (benzoylamino) hexyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
4-fluoro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (pyridin-2-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (2-hydroxy-2-methylpropionyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (7-oxo-7- { [ (3R) -tetrahydrofuran-3-ylmethyl ] amino } heptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 7-oxo-7- [ (tetrahydro-2H-pyran-4-ylmethyl) amino ] heptyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (azetidin-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (morpholin-4-ylmethyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-methylpiperazin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5- { [ (3-methylbutyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-hydroxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-chlorobenzoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [1 ' - (2-hydroxy-2-methylpropanoyl) -1 ', 2 ', 3 ', 6 ' -tetrahydro-2, 4 ' -bipyridin-5-yl ] -1, 3 ' -dihydro-2H-isoindole;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {1 '[ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [1 ' - (2-hydroxy-2-methylpropanoyl) -1 ', 2 ', 3 ', 6 ' -tetrahydro-3, 4 ' -bipyridin-6-yl ] -1, 3 ' -dihydro-2H-isoindole;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-aminoethyl) -1H-imidazol-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2, 2-dimethyl-1, 3-dioxolan-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-methoxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4S) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4R) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } -2-oxoethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3- { benzyl [3- (morpholin-4-yl) propyl ] amino } -3-oxopropyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (6-bromo-2-oxoquinolin-1 (2H) -yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [6- (3-acetylphenyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (morpholin-4-ylacetyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (morpholin-4-ylacetyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (2- { (4-fluorobenzyl) [4- (pyridin-3-yl) benzyl ] amino } -1, 3-thiazol-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2-benzyl-1, 3-thiazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (7- { benzyl [3- (morpholin-4-yl) propyl ] amino } -7-oxoheptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-thiazol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (4-methylphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-dihydroxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (ethanesulfonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2, 3-dihydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1-hydroxy-4-methylpent-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (5- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.3] hept-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.4] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 9-diazaspiro [5.5] undecan-3-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { benzyl [3- (morpholin-4-yl) propyl ] amino } -4-oxobutyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4-phenylbutyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetyl-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butyrylamino) phenyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (3S) -pyrrolidin-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methoxybenzyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (2-oxa-7-azaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [6- (3-acetylphenyl) -4- (3-hydroxypropyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5- (acetamidomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {5- [2- (2-chlorobenzyl) -1, 3-thiazol-4-yl ] -2-thienyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-fluorophenyl) butyl ] -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (3R) -1-isobutyrylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-benzoylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (methylsulfonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-isobutylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (2-hydroxypropan-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
{4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzyl } carbamic acid tert-butyl ester;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (methoxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5- { [ (tetrahydrofuran-2-ylmethyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-methoxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (5- { [4- (2-methoxyethyl) piperazin-1-yl ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole;
N- [4- ({ [1- (morpholin-4-yl) cyclopentyl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-pentanoylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (1-acetylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (1-isobutyrylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl (2- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } ethyl) carbamate;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (4, 4, 4-trifluorobutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-phenylpropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (phenylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxyphenyl) acetyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclopropylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-benzoylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-ethoxypropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (1-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpiperidin-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl [ (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } azetidin-3-yl) methyl ] carbamate;
n- (4- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (morpholin-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (2, 3-dimethylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3, 3-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tricyclo [ 3.3.1.1-3, 7- ] decan-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxycyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [4- (acetylamino) phenyl ] sulfonyl } amino) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (propylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-propylphenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (butanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ ({ [ (1S, 4R) -7, 7-dimethyl-2-oxobicyclo [2.2.1] hept-1-yl ] methyl } sulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (benzylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-fluorophenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (thiophen-2-ylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (N, N-dimethylglycyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (4, 4-difluorocyclohexyl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (piperidin-1-ylsulfonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [1- (1, 3-thiazol-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -D-phenylpropanamide;
N- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (5-methyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-chloro-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (2-carbamoylbenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n2(Nalpha) - {4- [ (5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridin-6-ylcarbonyl) amino ] benzoyl } -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (4, 5, 6, 7-tetrahydro-1H-indazol-5-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-1-oxobutan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxyprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -1-cyanobutan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanocyclopropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (4-methyl-1, 3-thiazol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
1- {4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } azetidine-3-carboxylic acid methyl ester;
N- (4- {3- [ (3-methylbutyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (benzylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (cyclopentylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (cyclopentylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (2-methoxyethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopentylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrrolidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [ (dimethylamino) methyl ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 3-oxazol-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) (3-methylbutyryl) amino ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (9-chloro-5-oxo-2, 3, 3a, 4, 4a, 5-hexahydro-6H-furo [2 ', 3': 2, 3] cyclobuta [1, 2-c ] quinolin-6-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ 7-chloro-1- (2-hydroxyethyl) -3-oxo-1, 3-dihydrocyclobuta (cyclobuta) [ c ] quinolin-4 (2H) -yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (1-acetylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclopentylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (3, 5-dimethyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-difluoroethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -L-phenylalanine amide;
n- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiophen-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pyrimidin-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (5-oxo-L-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4, 4-difluorocyclohexyl) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (propan-2-yloxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-acetylpiperidin-4-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { 7-oxo-7- [ (3-phenylpropyl) amino ] heptyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (bicyclo [2.2.1] hept-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1, 3-thiazol-5-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-oxo-4, 5, 6, 7-tetrahydro-1-benzofuran-3-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {2- [ (3-methylbutyryl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (4-methylpentanoyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (ethoxyacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { [ (2-methoxyethoxy) acetyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-2-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [2- (benzoylamino) ethyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-3-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-L-prolyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-propionylazetidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pent-4-ynoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (thiophen-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethylglycyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethyl- β -alanyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrrolidin-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (pyrrolidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({1- [3- (piperidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methylpiperazin-1-yl) acetyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopropylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopentylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3-dimethylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (butanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (benzenesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-fluorophenyl) sulfonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propan-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (benzylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (thien-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -2-methylbutyryl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4, 4-difluorocyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-D-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (2-methylpentanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1, 2-oxazol-5-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridazin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrazin-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({1- [3- (piperidin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
trans-3- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] cyclobutanecarboxylic acid benzyl ester;
n- [4- (4- { [ (4-methylpiperazin-1-yl) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (benzoylamino) cyclohex-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (4- { [ (1-methylpiperidin-4-yl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydro-2H-thiopyran-4-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3R) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3S) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -2-methylbutyryl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (3-methylbutyryl) amino ] oxetan-3-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
4- ({4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } sulfonyl) piperidine-1-carboxylic acid tert-butyl ester;
n- {4- [4- (propylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methoxyethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (cyclopentylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (1, 4-dioxan-2-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopentylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (morpholin-4-ylcarbonyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopropylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [4- (but-2-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-dioxido-tetrahydro-2H-thiopyran-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { (4R) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (4S) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [ trans-3- (benzylcarbamoyl) cyclobutyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { trans-3- [ (2-phenylethyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { trans-3- [ (3-phenylpropyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methyl-1, 3-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (furan-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -3- (furan-2-yl) prop-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 3-oxazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (3, 3, 3-trifluoropropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 5-dimethyl-1H-pyrazol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methoxycyclohexyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 3-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-difluorocyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c1 pyridine-2-carboxamide;
n- {4- [1- (1H-pyrazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tert-butoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-1, 2, 4-triazol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (3-ethoxypropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-hydroxy-3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-pyrrol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methylpropoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1-methyl prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-hydroxycyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1- { [1- (methoxymethyl) cyclopropyl ] carbonyl } -1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (methylsulfonyl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-acetyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -4-methylpent-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-methoxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopent-1-en-1-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (thiophen-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1-methyl-1H-pyrrol-2-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (4-methylhexanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-dimethylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-5-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclobutylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (piperidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [2- (pyrrolidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3S) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({ (3S) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (bicyclo [2.2.1] hept-2-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { cis-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopentylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and pharmaceutically acceptable salts thereof.
Yet another embodiment relates to compounds of formula (Ic) which are:
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
Yet another embodiment relates to compounds of formula (Ic) which are:
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
Another embodiment relates to a composition for treating: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, dementia of the vascular or AD type, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct area and myocardial fibrosis, for preventing graft failure and cystic fibrosis, said composition comprising an excipient and a therapeutically effective amount of a compound of formula (Ic) or a pharmaceutically acceptable salt thereof.
Another embodiment relates to a composition for treating: inflammatory and tissue repair disorders; especially rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases, including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, in particular, wherein the cancer is selected from the group consisting of breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatosis, cachexia, inflammation associated with infection and certain viral infections, including acquired immunodeficiency syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia, said composition comprising an excipient and a therapeutically effective amount of a compound of formula (Ic) or a pharmaceutically acceptable salt thereof.
Another embodiment relates to a method of treating a patient for: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for preventing graft failure and cystic fibrosis, the method comprising: administering to the patient a therapeutically effective amount of a compound of formula (Ic) or a pharmaceutically acceptable salt thereof.
Another embodiment relates to a method of treating a patient for: inflammatory and tissue repair disorders; especially rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, in particular, wherein the cancer is selected from the group consisting of breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatosis, cachexia, inflammation associated with infection and certain viral infections including acquired immunodeficiency syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia, comprising: administering to the patient a therapeutically effective amount of a compound of formula (Ic) or a pharmaceutically acceptable salt thereof.
Another embodiment relates to a method of treating a patient for: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for preventing graft failure and cystic fibrosis, the method comprising: administering to the patient a therapeutically effective amount of a compound of formula (Ic) or a pharmaceutically acceptable salt thereof; and a therapeutically effective amount of one or more other therapeutic agents.
Another embodiment relates to a method of treating a patient for: inflammatory and tissue repair disorders; especially rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases, including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, in particular, wherein the cancer is selected from the group consisting of breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatosis, cachexia, inflammation associated with infection and certain viral infections, including acquired immunodeficiency syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia or spleen cancer, comprising: administering to the patient a therapeutically effective amount of a compound of formula (Ic) or a pharmaceutically acceptable salt thereof; and a therapeutically effective amount of one or more other therapeutic agents.
Detailed description of the invention
The purpose of the detailed description is only to acquaint others skilled in the art of applicant's invention with its principles and its practical application, so that others skilled in the art may modify and use the invention in many forms, such that they may be well suited to the requirements of a particular use. This description and its specific embodiments are intended for purposes of illustration only. Therefore, the present invention is not limited to the embodiments described in the patent application, and various modifications can be made.
Abbreviations and Definitions
Unless defined otherwise herein, scientific and technical terms used in connection with the present invention have the same meaning as commonly understood by one of ordinary skill in the art. The meaning and scope of the terms will be clear, however, if any potential ambiguity exists, the definitions provided herein take precedence over any dictionary or foreign definition. In this application, the use of "or" means "and/or" unless stated otherwise. Furthermore, the terms "including" (as well as other forms, such as "includes" and "including") are not limiting. As used in this application, including the claims, the words "comprise" or "containing" indicate that: unless the context requires otherwise, those words should be used on a clear understanding basis, they are to be interpreted inclusively rather than exclusively, and the applicant intends to so interpret each of those words in the course of interpreting this patent application, including the following claims. For a variable that occurs more than one time in any substituent or in a compound of the invention or any other formula herein, its definition on each occurrence is independent of its definition at other occurrences. Substituents may be combined, but such combination is required to produce stable compounds. A stable compound is a compound that can be isolated from a reaction mixture in useful purity.
It is understood that for all combinations herein, monovalent moieties having more than one atom are linked by their left ends, with divalent moieties drawn from left to right, maintaining appropriate valencies.
As used in this specification and the appended claims, the following terms have the indicated meanings, unless otherwise specified:
the term "alkyl" (alone or in combination with other terms) refers to a straight or branched chain saturated hydrocarbyl substituent, typically containing from 1 to about 10 carbon atoms; or in another embodiment, from 1 to about 8 carbon atoms; in another embodiment, from 1 to about 6 carbon atoms; in another embodiment, from 1 to about 4 carbon atoms. Examples of such substituents include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, and hexyl, and the like.
The term "alkenyl" (alone or in combination with other terms) refers to a straight or branched chain hydrocarbyl substituent containing one or more double bonds, typically from 2 to about 10 carbon atoms; or in another embodiment, from 2 to about 8 carbon atoms; in another embodiment, from 2 to about 6 carbon atoms; in another embodiment, from 2 to about 4 carbon atoms. Examples of such substituents include ethenyl, 2-propenyl, 3-propenyl, 1, 4-pentadienyl, 1, 4-butadienyl, 1-butenyl, 2-butenyl, 3-butenyl, and the like.
The term "alkynyl" (alone or in combination with other terms) refers to a straight or branched chain hydrocarbyl substituent containing one or more triple bonds, typically containing from 2 to about 10 carbon atoms; or in another embodiment, from 2 to about 8 carbon atoms; in another embodiment, from 2 to about 6 carbon atoms; in another embodiment, from 2 to about 4 carbon atoms. Examples of such substituents include ethynyl, 2-propynyl, 3-propynyl, 2-butynyl and 3-butynyl, and the like.
The term "carbocyclyl" (alone or in combination with other terms) refers to a saturated ring (i.e., "cycloalkyl"), a partially saturated ring (i.e., "cycloalkenyl"), or a fully unsaturated (i.e., "aryl") hydrocarbyl substituent containing from 3 to 14 carbon ring atoms (the "ring atoms" being the atoms which are joined together to form a ring substituent). Carbocyclyl groups may be monocyclic or polycyclic in structure.
Carbocyclyl groups may be monocyclic structures, typically containing 3 to 8 ring atoms, more typically 3 to 6 ring atoms, and even more typically 5 to 6 ring atoms. Examples of such monocyclic carbocyclic groups include cyclopropyl (cyclopropane), cyclobutyl (cyclobutane), cyclopentyl (cyclopentanyl), cyclopentenyl, cyclopentadienyl, cyclohexyl (cyclohexane), cyclohexenyl, cyclohexadienyl and phenyl. The carbocyclyl group may also be a polycyclic carbocyclyl group (i.e., may contain more than one ring). Examples of polycyclic carbocyclyl groups include bridged, fused and spirocyclic carbocyclyl groups. In a spiro carbocyclic group, two different rings share a common atom. An example of a spirocyclic carbocyclyl is spiropentyl. In a bridged carbocyclyl group, the rings share at least two non-adjacent atoms in common. Examples of bridged carbocyclyl groups include bicyclo [2.2.1] heptyl, bicyclo [2.2.1] hept-2-enyl, and adamantyl. In fused cyclic carbocyclic ring systems, two or more rings may be fused together such that the two rings share a common bond. Examples of two or three fused ring carbocyclic groups include naphthyl, tetrahydronaphthyl, indenyl, indanyl (indanyl), anthracenyl, phenanthrenyl and naphthylalkyl.
The term "cycloalkyl" (alone or in combination with other terms) refers to a saturated cyclic hydrocarbyl substituent containing from 3 to 14 carbon ring atoms. Cycloalkyl groups may be monocyclic, typically containing 3 to 8 carbon ring atoms, and more typically containing 3 to 6 ring atoms. Examples of monocyclic cycloalkyl groups include cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl. The cycloalkyl group can also be a polycyclic cycloalkyl group or a cycloalkyl group containing more than one ring. Examples of polycyclic cycloalkyl groups include bridged, fused, and spirocyclic carbocyclic groups. In bridged cycloalkyl groups, the rings share at least two non-adjacent atoms in common. Examples of bridged cycloalkyl groups include bicyclo [2.2.1] heptyl and adamantyl.
The term "aryl" (alone or in combination with other terms) refers to an aromatic carbocyclic group containing 6 to 14 carbon ring atoms. The aryl group can be a monocyclic or polycyclic aryl group (i.e., can contain more than one ring). In the case of polycyclic aromatic rings, only one ring in the polycyclic system is required to be an unsaturated ring, while the remaining rings may be saturated, partially saturated, or unsaturated. Examples of aryl groups include phenyl, naphthyl, indenyl, 2, 3-indanyl, indanyl and tetrahydronaphthyl.
In some instances, the number of carbon atoms in a hydrocarbyl substituent (e.g., alkyl, alkenyl, alkynyl, or cycloalkyl) is preceded by the prefix "Cx-Cy- "wherein x is the minimum number of carbon atoms in the substituent and y is the maximum number of carbon atoms in the substituent. Thus, for example, "C1-C6-alkyl "means an alkyl substituent containing from 1 to 6 carbon atoms. To further illustrate, C3-C8Cycloalkyl refers to a saturated hydrocarbon-based ring containing from 3 to 8 carbon ring atoms.
The term "hydrogen" (alone or in combination with other terms) refers to a hydrogen radical and may be written as — H.
The term "hydroxy" (alone or in combination with other terms) means-OH.
The term "carboxy" (alone or in combination with other terms) means-c (o) -OH.
The term "amino" (alone or in combination with other terms) means-NH2。
The term "halogen" or "halo" (alone or in combination with other terms) refers to a fluoro group (which may be written as-F), a chloro group (which may be written as-Cl), a bromo group (which may be written as-Br), or an iodo group (which may be written as-I).
If a substituent is described as "substituted," non-hydrogen radicals replace hydrogen radicals on carbon or nitrogen of the substituent. Thus, for example, a substituted alkyl substituent is an alkyl substituent in which at least one non-hydrogen radical replaces a hydrogen radical on the alkyl substituent. To illustrate, a monofluoroalkyl is an alkyl substituted with one fluoro group and a difluoroalkyl is an alkyl substituted with two fluoro groups. It will be appreciated that if more than one substitution is present on a substituent, each non-hydrogen radical may be the same or different (unless otherwise specified).
If a substituent is described as "optionally substituted," that substituent may be: (1) unsubstituted, or (2) substituted. If a substituent is described as being optionally substituted with up to a specific number of non-hydrogen radicals, that substituent may be: (1) unsubstituted; or (2) substituted at the substituent position with up to a specific number of non-hydrogen radicals, or with up to the maximum number of non-hydrogen radicals, but fewer. Thus, for example, if a substituent is described as a heteroaryl group optionally substituted with up to three non-hydrogen radicals, any heteroaryl group having less than three substitutable positions will optionally be substituted with up to as many non-hydrogen radicals as the heteroaryl group has substitutable positions. For example, tetrazolyl (which has only one substitutable position) is optionally substituted with up to one non-hydrogen radical. To further illustrate, if an amino nitrogen is described as being optionally substituted with up to 2 non-hydrogen radicals, then a primary amino nitrogen is optionally substituted with up to 2 non-hydrogen radicals, and a secondary amino nitrogen is optionally substituted with up to 1 non-hydrogen radical.
The terms "substituent" and "group" are used interchangeably herein.
The prefix "halo" indicates that the substituent to which the prefix is attached is substituted with one or more independently selected halogen groups. For example, haloalkyl refers to an alkyl substituent wherein at least one hydrogen radical is substituted with a halogen radical. Examples of the haloalkyl group include chloromethyl, 1-bromoethyl, fluoromethyl, difluoromethyl, trifluoromethyl and 1, 1, 1-trifluoroethyl. It will be appreciated that if a substituent is substituted with more than one halogen group, those halogen groups may be the same or different (unless otherwise specified).
The prefix "perhalo" indicates that each hydrogen radical on the substituent to which the prefix is attached is substituted with an independently selected halogen group, i.e., each hydrogen radical on the substituent is substituted with a halogen group. If all halogen groups are the same, the prefix generally indicates the halogen group. Thus, for example, the term "perfluoro" means that each hydrogen radical on the substituent to which the prefix is attached is replaced with a fluoro group. For purposes of this specification, the term "perfluoroalkyl" refers to an alkyl substituent group in which each hydrogen radical is replaced with a fluoro group.
The term "carbonyl" (alone or in combination with other terms) means-c (o) -.
The term "aminocarbonyl" (alone or in combination with other terms) means-C (O) -NH 2。
The term "oxo" (alone or in combination with other terms) refers to (═ O).
The term "oxy" (alone or in combination with other terms) refers to an ether substituent and may be written as-O-.
The term "alkylhydroxy" (alone or in combination with other terms) means-alkyl-OH.
The term "alkylamino" (alone or in combination with other terms) means-alkyl-NH2。
The term "alkoxy group"(alone or in combination with other terms) refers to an alkyl ether substituent, i.e., -O-alkyl. Examples of such substituents include: methoxy (-O-CH)3) Ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy and tert-butoxy.
The term "alkylcarbonyl" (alone or in combination with other terms) refers to-c (o) -alkyl.
The term "aminoalkylcarbonyl" (alone or in combination with other terms) means-C (O) -alkyl-NH2。
The term "alkoxycarbonyl" (alone or in combination with other terms) refers to-C (O) -O-alkyl.
The term "carbocyclylcarbonyl" (alone or in combination with other terms) refers to-c (o) -carbocyclyl.
Similarly, the term "heterocyclylcarbonyl" (alone or in combination with other terms) refers to-c (o) -heterocyclyl.
The term "carbocyclylalkylcarbonyl" (alone or in combination with other terms) refers to-c (o) -alkyl-carbocyclyl.
Similarly, the term "heterocyclylalkylcarbonyl" (alone or in combination with other terms) refers to-c (o) -alkyl-heterocyclyl.
The term "carbocyclyloxycarbonyl" (alone or in combination with other terms) refers to-C (O) -O-carbocyclyl.
The term "carbocyclylalkoxycarbonyl" (alone or in combination with other terms) refers to-c (O) -O-alkyl-carbocyclyl.
The term "thio" or "thia" (alone or in combination with other terms) refers to a thioether substituent, i.e., an ether substituent in which a divalent sulfur atom replaces an ether oxygen atom. Such substituents may be described as-S-. For example, such "alkyl-thio-alkyl" refers to alkyl-S-alkyl (alkyl-thio-alkyl).
The term "thiol" or "mercapto" (alone or in combination with other terms) refers to a mercapto substituent and may be written as — SH.
The term "(thiocarbonyl)" (alone or in combination with other terms) refers to a carbonyl group having an oxygen atom replaced with sulfur. Such substituents may be described as-C (S) -.
The term "sulfonyl" (alone or in combination with other terms) means-S (O)2-。
The term "aminosulfonyl" (alone or in combination with other terms) means-S (O)2-NH2。
The term "sulfinyl" or "sulfoxide" (alone or in combination with other terms) refers to-S (O) -.
The term "heterocyclyl" (alone or in combination with other terms) refers to a saturated (i.e., "heterocycloalkyl"), partially saturated (i.e., "heterocycloalkenyl") or fully unsaturated (i.e., "heteroaryl") ring structure containing a total of 3 to 20 ring atoms. At least one ring atom is a heteroatom (i.e., oxygen, nitrogen, or sulfur), and the remaining ring atoms are independently selected from carbon, oxygen, nitrogen, and sulfur. The heterocyclic group may be a monocyclic or polycyclic structure.
Heterocyclyl groups may be monocyclic heterocyclyl groups, which typically contain 3 to 7 ring atoms, more typically 3 to 6 ring atoms, and even more typically 5 to 6 ring atoms. Examples of monocyclic heterocyclic groups include: 1, 2, 3, 6-tetrahydropyridine, thiomorpholinyl, tetrahydropyranyl, furanyl, dihydrofuranyl, tetrahydrofuranyl, thienyl (thiofuranyl), dihydrothienyl, tetrahydrothienyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrrolidin-2-onyl, imidazolyl, imidazolinyl, imidazolidinyl, pyrazolyl, pyrazolinyl, pyrazolidinyl, triazolyl, tetrazolyl, oxazolyl, oxazolidinyl, isoxazolyl, thiazolyl, isothiazolyl, thiazolinyl, isothiazolinyl, thiazolidinyl, isothiazolidinyl, thiadiazolyl, oxadiazolyl (including 1, 2, 3-oxadiazolyl, 1, 2, 4-oxadiazolyl, 1, 2, 5-oxadiazolyl (furazanyl), or 1, 3, 4-oxadiazolyl), oxadiazolyl (including 1, 2, 3, 4-oxatriazolyl or 1, 2, 3, 5-oxatriazolyl), oxadiazolyl (including 1, 2, 3-dioxazolyl, 1, 2, 4-dioxazolyl, 1, 3, 2-dioxazolyl, or 1, 3, 4-dioxazolyl), thiazolyl, oxathiolanyl (oxathiolanyl), oxathiolanyl, pyranyl, dihydropyranyl, thiopyranyl, tetrahydrothiopyranyl, pyridyl (azinyl), piperidinyl, diazinyl (including pyridazinyl (1, 2-diazinyl), pyrimidinyl (1, 3-diazinyl) or pyrazinyl (1, 4-diazinyl)), piperazinyl, pyrrolidin-2-onyl (pyrolidin-2-only), triazinyl (including 1, 3, 5-triazinyl, 1, 2, 4-triazinyl, and 1, 2, 3-triazinyl)), oxazinyl (including 1, 2-oxazinyl, 1, 3-oxazinyl, or 1, 4-oxazinyl)), oxathiazinyl (including 1, 2, 3-oxathiazinyl, 1, 2, 4-oxathiazinyl, 1, 2, 5-oxathiazinyl, or 1, 2, 6-oxathiazinyl)), oxadiazinyl (including 1, 2, 3-oxadiazinyl, 1, 2, 4-oxadiazinyl, 1, 4, 2-oxadiazinyl, or 1, 3, 5-oxadiazinyl)), morpholinyl, aza-diazinylRadicals, oxacycloheptenyl (oxepinyl), thiepinyl (thiepinyl), diazaA group selected from the group consisting of thiomorpholinyl, tetrahydrothienyl 1, 1-dioxide (dioxinyl), tetrahydro-2H-thiopyranyl, 1, 1-dioxide (dioxinyl), oxetanyl, azetidinyl, thiazolyl, azepanyl, azepan-2-onyl and dioxolanyl (including 1, 3-dioxolanyl).
The heterocyclic group may also be a polycyclic heterocyclic group (i.e., may contain more than one ring). Examples of polycyclic heterocyclic groups include bridged, fused, and spirocyclic heterocyclic groups. In a spirocyclic heterocyclyl, two different rings share one atom. In a bridged heterocyclyl, the rings share at least two non-adjacent atoms in common. In fused cyclic heterocyclic groups, two or more rings may be fused together such that the two rings share a common bond. Examples of the condensed-ring heterocyclic group having two, three or four ringsThe sub-steps include: hexahydro-furo [3, 4-c ] s]Pyrrole, hexahydro-furo [3, 4-b ] compounds]Pyrrole, octahydro-pyrrolo [3, 4-b ] compounds]Pyridine, octahydro-pyrrolo [3, 4-c)]Pyridine, (3aR, 6aR) -5-methyl-octahydro-pyrrolo [3, 4-b)]Pyrrole, (3aR, 6aR) -octahydro-pyrrolo [3, 4-b)]Pyrrole, 6-methyl-2, 6-diaza-bicyclo [3.2.0]Heptane, (3aS, 6aR) -2-methyl-octahydro-pyrrolo [3, 4-c)]Pyrrole, decahydro- [1, 5]Naphthyridine, 2, 3-dihydrobenzofuranyl, 2, 3, 4, 9-tetrahydro-1H-pyrido [3, 4-b]Indolyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, isoindolin-1-one, phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b ][1，2]Diaza derivatives-4(5H) -keto, (trifluoromethyl) phthalazin-1 (2H) -keto, pyrrolo [1, 2-d][1，2，4]Triazine-1 (2H) -keto, 1, 2, 3, 4-tetrahydroisoquinolinyl, 2, 3-dihydrobenzo [ b][1，4]Dioxinyl, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -onyl, 5, 6, 7, 8-tetrahydro- [1, 2, 4 ]]Triazolo [4, 3-a]Pyrazinyl, 5, 6, 7, 8-tetrahydroimidazo [1, 5-a ]]Pyrazinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, indenylazinyl, pyranopyrrolyl, 4H-quinolizinyl, purinyl, naphthyridinyl, pyridopyridyl (including pyrido [3, 4-b ]]-pyridinyl, pyrido [3, 2-b ]]-pyridyl, or pyrido [4, 3-b]-pyridyl), pteridinyl, 4, 5, 6, 7-tetrahydro-indolyl, 5, 6, 7, 8-tetrahydroimidazo [1, 5-a ]]Pyrazinyl, 6, 7-dihydropyrrolo [3, 4-d ]]Pyrimidinyl, 6, 7-dihydropyrrolo [3, 4-b ]]Pyridyl, 2, 3-dihydropyrrolo [3, 4-c]Pyridyl, 6, 7-dihydrobenzofuran-4 (5H) -one, indolinyl, benzo [ d][1，3]Dioxolyl, isoquinolinyl, indolyl, quinolin-2 (1H) -onyl, benzo [ d ] o]Imidazolyl, 1, 2, 3, 4-tetrahydrocyclobuta (cyclobuta) [ c]Quinolyl, 1, 2-dihydrocyclobuta [ c ]Quinolin-3 (4H) -onyl, and 3, 3a, 4, 4 a-tetrahydro-2H-furo [2 ', 3': 2, 3]Cyclobutanea [1, 2-c ]]Quinoline-5 (6H) -keto group. Fused ring heteroOther examples of cyclic groups include: benzo-fused heterocyclic radicals, e.g. benzimidazolyl, benzo [ d][1，3]Dioxolyl, indolyl, isoindolyl (isobenzoxazolyl, pseudoisoindolyl), isoindolyl (isoindolyl), isoindolyl (phenyl pyrazolyl), benzazinyl (including quinolyl (1-benzazinyl) or isoquinolyl (2-benzazinyl)), phthalazinyl, quinoxalinyl, quinazolinyl, benzodiazinyl (including cinnolinyl (1, 2-benzodiazinyl) or quinazolinyl (1, 3-benzodiazinyl)), benzopyranyl (including chromanyl or isobenzopyranyl), benzoxazinyl (including 1, 3, 2-benzoxazinyl, 1, 4, 2-benzoxazinyl, 2, 3, 1-benzoxazinyl, or 3, 1, 4-benzoxazinyl), benzisoxazinyl (including 1, 2-benzisoxazinyl or 1, 4-benzisoxazinyl), isoindolin-1-one, 2, 3-dihydrobenzo [ b ]][1，4]Dioxinyl, 1, 2, 3, 4-tetrahydroisoquinolinyl, quinolin-2 (1H) -onyl, benzo [ d ] ]Imidazolyl, 2, 3, 4, 9-tetrahydro-pyrido [3, 4-b ]]Indolyl, 1, 2, 3, 4-tetrahydrocyclobuta (cyclobuta) [ c]Quinolyl, 1, 2-dihydrocyclobuta [ c]Quinoline-3 (4H) -keto and 3, 3a, 4, 4 a-tetrahydro-2H-furo [2 ', 3': 2, 3]Cyclobutanea [1, 2-c ]]Quinoline-5 (6H) -keto group. Examples of spirocyclic heterocyclic groups include: 1, 4-dioxa-8-azaspiro [4.5 ]]Decyl, 2-oxa-6-aza-spiro [3.3]Heptyl, bicyclo [2.2.1]Heptane-2-oxo, 6-oxa-1-aza-spiro [3.3]Heptyl, 2-oxa-7-aza-spiro [3.5 ]]Nonyl, 2-oxa-6-aza-spiro [3.5]Nonyl, 2-oxa-5-aza-spiro [3.5]Nonyl, 2-oxa-6-aza-spiro [3.4]Octyl, 2-oxa-5-aza-spiro [3.4]Octyl, 2, 7-diazaspiro [3.5 ]]Nonane, 1, 4-dioxa-8-azaspiro [4.5 ]]Decyl, 2-oxa-9-azaspiro [5.5]Undecyl, 2, 9-diazaspiro [5.5]Undecyl, 2, 8-diazaspiro [5.5]Undecyl, 1-oxa-8-azaspiro [5.5]Undecyl, 1, 8-diazaspiro [5.5]Undecyl, 3, 9-diazaspiro [5.5]Undecyl, 1-oxa-4, 8-diazaspiro [5.5]Undecyl, 1, 8-diazaspiro [4.6 ]]Undecyl, 1-oxa-8-azaspiro [4.5 ]Decyl, 2, 7-diazaspiro [4.5]]Decyl, 1, 8-diazaspiro [4.5]]The number of decyl groups, 2,8-diazaspiro [4.5]]Decyl, 2, 6-diazaspiro [4.5]]Decyl, 1, 4-dioxaspiro [4.5]]Decyl, 1, 7-diazaspiro [4.4]]Nonyl, 2, 7-diazaspiro [4.4]]Nonyl, 2, 5-diazaspiro [3.5]]Nonyl, 2, 6-diazaspiro [3.5]]Nonyl, 1, 7-diazaspiro [3.5]]Nonyl, 6-oxa-2-azaspiro [3.5]]Nonyl, 1, 6-diazaspiro [3.5]]Nonyl, 2, 6-diazaspiro [3.4]]Octyl, 6-oxa-2-azaspiro [3.4]]Octyl, 5-oxa-2-azaspiro [3.4]Octyl and 2, 6-diazaspiro [3.3]]A heptyl group.
The term "heterocycloalkyl" (alone or in combination with other terms) refers to a saturated heterocyclic group. Examples of heterocycloalkyl groups include: piperidine, tetrahydropyranyl, piperazinyl, morpholinyl, azepan-2-onyl, pyrrolidinyl, 1, 3-dioxolanyl, tetrahydrofuranyl, pyrrolidin-2-onyl, oxetanyl, azetidinyl, 2-oxa-9-azaspiro [5.5] undecyl, 2, 9-diazaspiro [5.5] undecyl, 2, 8-diazaspiro [5.5] undecyl, 1-oxa-8-azaspiro [5.5] undecyl, 1, 8-diazaspiro [5.5] undecyl, 3, 9-diazaspiro [5.5] undecyl, 1-oxa-4, 8-diazaspiro [5.5] undecyl, 1, 8-diazaspiro [4.6] undecyl, 1-oxa-8-azaspiro [4.5] decyl, 2, 7-diazaspiro [4.5] decyl, 1, 8-diazaspiro [4.5] decyl, 2, 6-diazaspiro [4.5] decyl, 1, 4-diazaspiro [4.5] decyl, 1, 7-diazaspiro [4.4] nonyl, 2, 5-diazaspiro [3.5] nonyl, 2, 6-diazaspiro [3.5] nonyl, 1, 7-diazaspiro [3.5] nonyl, 6-oxa-2-azaspiro [3.5] nonyl, 1, 6-diazaspiro [3.5] nonyl, 2, 6-diazaspiro [3.4] octyl, 6-oxa-2-azaspiro [3.4] octyl, 5-oxa-2-azaspiro [3.4] octyl, bicyclo [2.2.1] heptan-2-onyl, 1, 4-dioxa-8-azaspiro [4.5] decyl, 2, 7-diazaspiro [3.5] nonyl and 2, 6-diazaspiro [3.3] heptyl.
The term "heteroaryl" (alone or in combination with other terms) refers to an aromatic heterocyclic group containing 5 to 14 ring atoms. Heteroaryl groups may be monocyclic or polycyclic heteroaryl (i.e., may contain more than one ring). In the case of polycyclic heteroaryl groups, only one heterocyclyl ring in a polycyclic ring system is required to be an unsaturated ring, while the remaining rings may be saturated, partially saturated, or unsaturated rings. Examples of heteroaryl substituents include: 6-membered ring substituents, for example pyridyl, pyrazinyl (pyrazyl), pyrrolyl, isoxazolyl, 1, 2, 3-triazolyl, pyrimidinyl, pyridazinyl and 1, 3, 5-, 1, 2, 4-or 1, 2, 3-triazinyl; 5-membered ring substituents such as imidazolyl, furyl, thienyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, 1, 2, 3-, 1, 2, 4-, 1, 2, 5-and 1, 3, 4-oxadiazolyl and isothiazolyl; 6/5 membered fused ring substituents such as indolyl, benzothiofuranyl, benzisoxazolyl, benzoxazolyl, purinyl, 4, 5, 6, 7-tetrahydro-indolyl, furo [3, 2-c ] pyridinyl, pyrrolo [1, 2-d ] [1, 2, 4] triazin-1 (2H) -one, thieno [3, 2-c ] pyridinyl, 5, 6, 7, 8-tetrahydroimidazo [1, 5-a ] pyrazinyl, benzo [ d ] imidazolyl, 6, 7-dihydro-pyrrolo [3, 4-d ] pyrimidinyl, 6, 7-dihydro-pyrrolo [3, 4-b ] pyridinyl, 2, 3-dihydro-pyrrolo [3, 4-c ] pyridinyl, 5, 6, 7, 8-tetrahydroimidazo [1, 5-a ] pyrazinyl, 6, 7-dihydrobenzofuran-4 (5H) -keto, and indolyl; 6/6 membered fused rings, for example benzopyranyl, quinolinyl, isoquinolinyl, cinnolinyl, quinazolinyl, benzoxazinyl, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, phthalazin-1 (2H) -one, isoquinolin-1 (2H) -one and quinolin-2 (1H) -one; 6/5/6 membered rings, for example 2, 3, 4, 9-tetrahydro-1H-pyrido [3, 4-b ] indolyl and 1, 2-dihydrocyclobuta (cyclobuta) [ c ] quinolin-3 (4H) -onyl; and 6/6/4/5 membered rings, for example, 2, 3, 4, 9-tetrahydro-pyrido [3, 4-b ] indolyl.
The prefix connecting substituents of the multiple moieties applies only to the first moiety. For example, the term "alkylcycloalkyl" contains two moieties: alkyl and cycloalkyl groups. Thus, C1-C6C on alkylcycloalkyl1-C6-prefix means: the alkyl moiety of an alkylcycloalkyl group contains 1 to 6 carbon atoms; c1-C6The prefix does not describe a cycloalkyl moiety. Further illustrateThe prefix "halo" on haloalkoxyalkyl means: only the alkoxy moiety of an alkoxyalkyl substituent is substituted with one or more halo groups. If halogen substitution can alternatively or additionally occur on the alkyl moiety, the substituent is instead described as "halogen-substituted alkoxyalkyl" rather than "haloalkoxyalkyl". Finally, if halogen substitution occurs only on the alkyl moiety, the substituent is instead described as "alkoxy haloalkyl".
The term "treatment" refers to a method of reducing or eliminating a disease and/or its attendant symptoms.
The term "prevention" refers to a method of preventing the onset of a disease and/or its attendant symptoms or avoiding afflicting a patient. As used herein, "preventing" also includes delaying the onset of the disease and/or its attendant symptoms and reducing the risk of getting ill in a patient.
The term "therapeutically effective amount" means: an amount of the compound administered sufficient to prevent or alleviate to some extent one or more symptoms of the condition or disorder being treated.
The term "modulate" refers to the ability of a compound to increase or decrease the function or activity of a kinase. As used herein, various forms of "modulation" include antagonism, agonism, partial antagonism and/or partial agonism of the activity associated with the kinase. Kinase inhibitors are compounds that, for example, bind to, partially or completely block stimulation, reduce, prevent, delay activation, inactivate, or down-regulate signal transduction. Kinase activators are compounds that, for example, bind, stimulate, elevate, open, activate, facilitate, enhance activation, sensitize, or up regulate signal transduction.
The term "composition" as used herein includes a product comprising the specified ingredients in the specified amounts, as well as any product which results, directly or indirectly, from combination of the specified ingredients in the specified amounts. By "pharmaceutically acceptable" it is meant that the carrier, diluent or excipient must not contradict the other components of the formulation and be deleterious to the recipient thereof.
As defined herein, a "patient" includes an animal, such as a mammal, including but not limited to: primates (e.g., humans), cows, sheep, goats, horses, dogs, cats, rabbits, rats, mice, and the like. In a preferred embodiment, the patient is a human.
Isotopically enriched or labelled compounds
The compounds of the present invention may exist in isotopically labeled or enriched forms, containing one or more atoms having an atomic mass or mass number different from the atomic mass or mass number of the atom most commonly found in nature. The isotope may be a radioactive or non-radioactive isotope. Isotopes of atoms (e.g., hydrogen, carbon, phosphorus, sulfur, fluorine, chlorine, and iodine) include, but are not limited to:2H，3H，13C，14C，15N，18O，32p，35S，18F，36cl and125I. compounds containing other isotopes of these and/or other atoms are within the scope of the present invention.
In another embodiment, the isotopically-labeled compound comprises deuterium (I)2H) Tritium (a)3H) Or14Isotope of C. Isotopically-labeled compounds of the present invention can be prepared by conventional methods well known to those skilled in the art. Such isotopically labeled compounds can be conveniently prepared by employing the procedures disclosed in the examples and schemes disclosed herein by substituting a readily available isotopically labeled reagent for a non-labeled reagent. In some cases, the compounds may be treated with isotopically-labelled reagents to exchange normal atoms for their isotopes, for example, in deuterium-containing acids such as D 2SO4/D2Under the action of O, hydrogen can be replaced by deuterium. In addition to the above methods, related methods and intermediates are disclosed in the following: for example, Lizondo, J et al, Drugs Fut, 21(11), 1116 (1996); brickner, S J et al, J Med Chem, 39(3), 673 (1996); mallesham, B et al, Org Lett, 5(7), 963 (2003); PCT patent applicationPublications WO1997010223, WO2005099353, WO1995007271, WO 2006008754; U.S. patent nos. 7538189; 7534814, respectively; 7531685, respectively; 7528131, respectively; 7521421, respectively; 7514068, respectively; 7511013, respectively; and U.S. patent application publication nos. 20090137457; 20090131485, respectively; 20090131363, respectively; 20090118238, respectively; 20090111840, respectively; 20090105338, respectively; 20090105307, respectively; 20090105147, respectively; 20090093422, respectively; 20090088416, respectively; and 20090082471, which are incorporated herein by reference.
Isotopically-labeled compounds of the present invention can be used as standards for determining the effectiveness of a Bcl-2 inhibitor in a binding assay. In drug studies, compounds containing isotopes have been used to study the in vivo metabolic fate of compounds by assessing the mechanism of action and metabolic pathways of non-isotopically labeled parent compounds (Blake et al J.pharm.Sci.64, 3, 367 (1975)). This metabolic study is important in the design of safe and effective therapeutic drugs, either because the active compound administered to the patient in vivo or because metabolites produced by the parent compound prove to be toxic or carcinogenic (Foster et al, Advances in Drug research Vol.14, pp.2-36, Academic press, London, 1985; Kato et al, J.Labelled Comp.Radiopharmaceut., 36 (10): 927-932 (1995); Kushner et al, Can.J.Physiol.Pharmacol., 77, 79-88 (1999)).
In addition, non-radioactive isotope-containing drugs, such as deuterated drugs known as "heavy drugs," can be used to treat diseases and conditions associated with Bcl-2 activity. The presence of an isotope in a compound in an amount above its natural abundance is referred to as enrichment. Examples of enrichment amounts include: about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 21, 25, 29, 33, 37, 42, 46, 50, 54, 58, 63, 67, 71, 75, 79, 84, 88, 92, 96 to about 100 mol%. In mammals, including rodents and dogs, up to about 15% of normal atoms have been replaced with heavy isotopes and for periods ranging from days to weeks, minimal side effects have been observed (Czajka D M and Finkel A J, Ann.N.Y.Acad.Sci.196084: 770; Thomson J F, Ann.New York Acad.Sci 196084: 736; Czakja D M et al, am.J.Physiol.1961201: 357). No toxicity was found in human fluids with acute replacement of up to 15% -23% by deuterium (Blagojevic N et al, "diagnosis & Treatment Planning for Neutron Capture Therapy", Zamenhof R, Solares G and Harling O eds.1994.advanced medical publishing, Madison Wis. pp. 125-134; Diabetes Metab. 23: 251 (1997)).
Labeling a drug with a stable isotope can change its physicochemical properties, such as pKa and lipid solubility. These effects and changes can affect the pharmacodynamic response of the drug molecule if isotopic substitution affects the regions involved in the ligand-receptor interaction. Although some of the physical properties of the stable isotope labeled molecules differ from those of the unlabeled molecules, the chemical and biological properties are the same, an important difference being: due to the increased mass of the heavy isotope, the heavy isotope binds to another atom more strongly than the light isotope binds to the same atom. Thus, the incorporation of isotopes at the site of metabolic or enzymatic conversion, relative to non-isotopic compounds, slows the reaction, potentially altering pharmacokinetic properties or effects.
Compound (I)
In the compounds of formula (I), X is independently selected1、X2、X3And R2A suitable group of (a). The described embodiments of the invention may be combined. All such combinations are included within the scope of the present invention. For example, any X1、X2、X3And R2Embodiments of (2) can be combined with any other X1、X2、X3And R2The defined combination of embodiments.
Embodiments of formula (I)
Accordingly, one embodiment of the present invention is directed to compounds, or pharmaceutically acceptable salts thereof, useful as inhibitors of NAMPT, the compounds having formula (I)
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3，C(O)OHOr C (O) NH2；
R2Is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r4，OR4，SR4，S(O)R4，SO2R4，C(O)R4，CO(O)R4，OC(O)R4，OC(O)OR4，NH2，NHR4，N(R4)2，NHC(O)R4，NR4C(O)R4，NHS(O)2R4，NR4S(O)2R4，NHC(O)OR4，NR4C(O)OR4，NHC(O)NH2，NHC(O)NHR4，NHC(O)N(R4)2，NR4C(O)NHR4，NR4C(O)N(R4)2，C(O)NH2，C(O)NHR4，C(O)N(R4)2，C(O)NHOH，C(O)NHOR4，C(O)NHSO2R4，C(O)NR4SO2R4，SO2NH2，SO2NHR4，SO2N(R4)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each phenyl group is optionally substituted at the para position with a group independently selected from: r5，OCH2CH2CH2CH2CH2CH3，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each phenyl is optionally substituted with one F; wherein each heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein R is2Is other than 4-methylphenyl;
R3is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R4is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r7，OR7，SR7，S(O)R7，SO2R7，C(O)R7，CO(O)R7，OC(O)R7，OC(O)OR7，NH2，NHR7，N(R7)2，NHC(O)R7，NR7C(O)R7，NHS(O)2R7，NR7S(O)2R7，NHC(O)OR7，NR7C(O)OR7，NHC(O)NH2，NHC(O)NHR7，NHC(O)N(R7)2，NR7C(O)NHR7，NR7C(O)N(R7)2，C(O)NH2，C(O)NHR7，C(O)N(R7)2，C(O)NHOH，C(O)NHOR7，C(O)NHSO2R7，C(O)NR7SO2R7，SO2NH2，SO2NHR7，SO2N(R7)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each aryl and heterocyclyl is optionally substituted with one or more groups independently selected from: r 8，OR8，SR8，S(O)R8，SO2R8，C(O)R8，CO(O)R8，OC(O)R8，OC(O)OR8，NH2，NHR8，N(R8)2，NHC(O)R8，NR8C(O)R8，NHS(O)2R8，NR8S(O)2R8，NHC(O)OR8，NR8C(O)OR8，NHC(O)NH2，NHC(O)NHR8，NHC(O)N(R8)2，NR8C(O)NHR8，NR8C(O)N(R8)2，C(O)NH2，C(O)NHR8，C(O)N(R8)2，C(O)NHOH，C(O)NHOR8，C(O)NHSO2R8，C(O)NR8SO2R8，SO2NH2，SO2NHR8，SO2N(R8)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R7is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r11，OR11，SR11，S(O)R11，SO2R11，NHR11，N(R11)2，C(O)R11，C(O)NH2，C(O)NHR11，C(O)N(R11)2，NHC(O)R11，NR11C(O)R11，NHSO2R11，NHC(O)OR11，SO2NH2，SO2NHR11，SO2N(R11)2，NHC(O)NH2，NHC(O)NHR11，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R8is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r12，OR12，SR12，S(O)R12，SO2R12，NHR12，N(R12)2，C(O)R12，C(O)NH2，C(O)NHR12，C(O)N(R12)2，NHC(O)R12，NR12C(O)R12，NHSO2R12，NHC(O)OR12，SO2NH2，SO2NHR12，SO2N(R12)2，NHC(O)NH2，NHC(O)NHR12，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: OCH (OCH)3Or an aryl group;
R10is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R11Is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R12is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, cycloalkyl or cycloalkenyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，CO(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]The pyridyl, pyrrolidin-2-one, cycloalkyl, and cycloalkenyl groups are optionally substituted with one or more groups independently selected from the group consisting of: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: NH (NH) 2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; and
R15is an alkyl group.
In one embodiment of formula (I), X1、X2And X3Is CH; x1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N. In another embodiment of formula (I), X1、X2And X3Is CH. In another embodiment of formula (I), X1And X3Is CH; x2Is N. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1. In another embodiment of formula (I), X2Is CH; x1And X3Is N. In another embodiment of formula (I), X2And X3Is CH; x1Is N.
In another embodiment of formula (I), R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (I), R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), R1Is R3(ii) a Wherein R is 3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In the formula (I)) In another embodiment of (1), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), R 1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), R1Is C (O) NH2. In another embodiment of formula (I), R1Is F. In another embodiment of formula (I), R1Is Cl. In another embodiment of formula (I), R1Is Br. In another embodiment of formula (I), R1Is CN. In another embodiment of formula (I), R1Is NH2. In another embodiment of formula (I), R1Is NO2. In another embodiment of formula (I), R1Is CF3. In another embodiment of formula (I), R1Is C (O) OH.
In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another of the formula (I)In one embodiment, X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is 3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by oneOr a plurality of groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (I), X1And X3Is CH; x2Is CR1；R1Is C (O) OH.
In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (I), X 2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6
OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (I), X 2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (I), X2And X3Is CH; x1Is CR1；R1Is C (O) OH.
In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (I), X1Is CH; x2And X 3Is CR1；R1Is Br. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (I), X1Is CH; x2And X3Is CR1；R1Is C (O) OH.
In one embodiment of formula (I),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N;
R1is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R2is alkyl, phenyl, heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r4，OR4，C(O)R4，CO(O)R4，NHC(O)R4，C(O)NHR4F, Cl, Br or I; each phenyl group is optionally substituted at the para position with a group independently selected from: r5，OCH2CH2CH2CH2CH2CH3，C(O)R5，NHR5，NHC(O)R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2Or CF3(ii) a Wherein each phenyl is optionally substituted with one F; wherein each heterocyclyl is optionally substituted with one or more groups independently selected from: r5，C(O)R5，NHC(O)R5，C(O)NHR5F, Cl, Br or I; wherein R is2Is other than 4-methylphenyl;
R3is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2OH, F, Cl, Br or I;
R4is alkyl, aryl or heterocyclyl; wherein each alkyl group is optionally independently selected by one or moreSubstituted with a group selected from: r7F, Cl, Br or I; wherein each aryl and heterocyclyl is optionally substituted with one or more groups independently selected from: r8，C(O)R8F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，C(O)NH2，C(O)OH，OH，CN，CF3F, Cl, Br or I;
R6is an alkyl or heterocyclic group;
R7is an aryl group;
R8is alkyl, aryl or heterocyclyl;
R9is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OCH (OCH)3Or an aryl group;
wherein R is3、R5、R6、R7、R8And R9The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13is alkyl, aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, or pyrrolidin-2-onyl wherein each alkyl is optionally substituted with one or more groups independently selected from And (3) substitution: r14，OR14，NH2OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]The pyridyl, pyrrolidin-2-one, cycloalkyl, and cycloalkenyl groups are optionally substituted with one or more groups independently selected from the group consisting of: r15，OR15，C(O)R15，CN，CF3F, Cl, Br or I;
R14is alkyl, aryl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OH, F, Cl, Br or I; and
R15is an alkyl group.
Yet another embodiment relates to compounds of formula (I) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 105, 106, 105, 102, 107, 110, 114, 111, 114, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 357, 358, 359, 360, 361, 362, 363, 364, 365, 366, 367, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454, 455, and pharmaceutically acceptable salts thereof.
Embodiments of formula (II)
In another aspect, the invention provides a compound of formula (II)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3As described herein for formula (I); r2Is phenylHeterocyclyl, cycloalkyl or cycloalkenyl; wherein the phenyl, heterocyclyl, cycloalkyl and cycloalkenyl groups are optionally substituted as described herein for formula (I).
In one embodiment of formula (II), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N. In another embodiment of formula (II), X1、X2And X3Is CH. In another embodiment of formula (II), X1And X3Is CH; x2Is N. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1. In another embodiment of formula (II), X2Is CH; x1And X3Is N. In another embodiment of formula (II), X2And X3Is CH; x1Is N.
In another embodiment of formula (II), R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (II), R 1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is 6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), R1Is C (O) NH2. In another embodiment of formula (II), R1Is F. In another embodiment of formula (II), R1Is Cl. In another embodiment of formula (II), R1Is Br. In another embodiment of formula (II), R1Is CN. In another embodiment of formula (II), R1Is NH2. In another embodiment of formula (II), R1Is NO2. In another embodiment of formula (II), R1Is CF3. In another embodiment of formula (II), R1Is C (O) OH.
In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (II), X 1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (II), X 1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (II), X1And X3Is CH; x2Is CR1；R1Is C (O) OH.
In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (II), X2And X3Is CH; x 1Is CR1；R1Is Br. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (II), X2And X3Is CH; x1Is CR1；R1Is C (O) OH.
In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (II), X 1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (II), X1Is CH; x2And X3Is CR1；R1Is C (O) OH.
In one embodiment of formula (II),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N;
R1is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R2is phenyl orA heterocyclic group; wherein each phenyl group is optionally substituted at the para position with one group independently selected from: r5，OCH2CH2CH2CH2CH2CH3，C(O)R5，NHR5，NHC(O)R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2Or CF3(ii) a Wherein each phenyl is optionally substituted with one F; wherein each heterocyclyl is optionally substituted with one or more groups independently selected from: r 5，C(O)R5，NHC(O)R5，C(O)NHR5F, Cl, Br or I; wherein R is2Is other than 4-methylphenyl;
R3is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2OH, F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，C(O)NH2，C(O)OH，OH，CN，CF3F, Cl, Br or I;
R6is an alkyl or heterocyclic group;
R9is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OCH (OCH)3Or an aryl group;
wherein R is3、R5、R6And R9The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13is alkyl, aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more groups independently selected from: r14，OR14，NH2OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] ]Pyridyl, furo [3, 2-c ]]The pyridyl, pyrrolidin-2-one, cycloalkyl, and cycloalkenyl groups are optionally substituted with one or more groups independently selected from the group consisting of: r15，OR15，C(O)R15，CN，CF3F, Cl, Br or I;
R14is alkyl, aryl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OH, F, Cl, Br or I; and
R15is an alkyl group.
Yet another embodiment relates to compounds of formula (II) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 105, 106, 102, 105, 107, 110, 114, 111, 114, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 452, 453, 454, 455, and pharmaceutically acceptable salts thereof.
Embodiments of formula (III)
In another aspect, the invention provides a compound of formula (III)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3As described herein for formula (I); when R is2When it is phenyl, RXAs described herein for formula (I).
In one embodiment of formula (III), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N. In another embodiment of formula (III), X1、X2And X3Is CH. In another embodiment of formula (III), X1And X3Is CH; x2Is N. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1. In another embodiment of formula (III), X2Is CH; x1And X3Is N. In another embodiment of formula (III), X2And X3Is CH; x1Is N.
In another embodiment of formula (III), R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In the formula (III)In another embodiment, R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted Substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), R1Is C (O) NH2. In another embodiment of formula (III), R1Is F. In another embodiment of formula (III), R1Is Cl. In another embodiment of formula (III), R1Is Br. In another embodiment of formula (III), R1Is CN. In another embodiment of formula (III), R1Is NH2. In another embodiment of formula (III), R1Is NO2. In another embodiment of formula (III), R1Is CF3. In another embodiment of formula (III), R1Is C (O) OH.
In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from And (3) substitution: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X 1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from：R6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (III), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (III), X 1And X3Is CH; x2Is CR1；R1Is C (O) OH.
In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III)，X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (III), X2And X 3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of the formula (III)In the embodiment, X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (III), X2And X3Is CH; x1Is CR1；R1Is C (O) OH.
In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is OR 3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; each of whichAlkyl is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (III), X1Is CH; x2And X3Is CR1；R1Is C (O) OH.
In another embodiment of formula (III), RxIs phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b][1，2]Diaza-4 (5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, or pyrrolo [1, 2-d ]][1，2，4]Triazin-1 (2H) -ones.
In one embodiment of formula (III),
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N;
R1is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
RXis R5，OCH2CH2CH2CH2CH2CH3，C(O)R5，NHR5，NHC(O)R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CF3Or F;
R3is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2OH, F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，C(O)NH2，C(O)OH，OH，CN，CF3F, Cl, Br or I;
R6is an alkyl or heterocyclic group;
R9is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OCH (OCH)3Or an aryl group;
wherein R is3、R5、R6And R9The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13is alkyl, aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more groups independently selected from: r 14，OR14，NH2OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]The pyridyl, pyrrolidin-2-one, cycloalkyl, and cycloalkenyl groups are optionally substituted with one or more groups independently selected from the group consisting of: r15，OR15，C(O)R15，CN，CF3F, Cl, Br or I;
R14is alkyl, aryl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OH, F, Cl, Br or I; and
R15is an alkyl group.
Yet another embodiment relates to compounds of formula (III) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 105, 106, 105, 102, 107, 110, 114, 111, 114, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 330, 331, 332, 333, 336, 337, 338, 339, 340, 341, 342, 343, 348, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 547, 548, 549, 550, 551, 552, and pharmaceutically acceptable salts thereof.
Embodiments of formula (IV)
In another aspect, the invention provides a compound of formula (IV):
or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3And R5As described herein for formula (I).
In one embodiment of formula (IV), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N. In another embodiment of formula (IV), X1、X2And X3Is CH. In another embodiment of formula (IV), X1And X3Is CH; x2Is N. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IV), X2Is CH; x1And X3Is N. In another embodiment of formula (IV), X2And X3Is CH; x1Is N.
In another embodiment of formula (IV), R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IV), R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionallySubstituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), R1Is C (O) NH2. In another embodiment of formula (IV), R1Is F. In another embodiment of formula (IV), R1Is Cl. In another embodiment of formula (IV), R1Is Br. In another embodiment of formula (IV), R1Is CN. In another embodiment of formula (IV), R1Is NH2. In another embodiment of formula (IV), R1Is NO2. In another embodiment of formula (IV), R1Is CF3. In another embodiment of formula (IV), R1Is C (O) OH.
In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X 1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IV), X1And X3Is CH; x2Is CR1；R1Is C (O) OH.
In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IV), X 2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IV), X 2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IV), X2And X3Is CH; x1Is CR1；R1Is C (O) OH.
In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IV), X1Is CH; x 2And X3Is CR1；R1Is Br. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IV), X1Is CH; x2And X3Is CR1；R1Is C (O) OH.
In one embodiment of formula (IV),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N;
R1is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R3is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2OH, F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，C(O)NH2，C(O)OH，OH，CN，CF3F, Cl, Br or I;
R6is an alkyl or heterocyclic group;
R9is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OCH (OCH) 3Or an aryl group;
wherein R is3、R5、R6And R9The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13is alkyl, aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more groups independently selected from: r14，OR14，NH2OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]The pyridyl, pyrrolidin-2-one, cycloalkyl, and cycloalkenyl groups are optionally substituted with one or more groups independently selected from the group consisting of: r15，OR15，C(O)R15，CN，CF3F, Cl, Br or I;
R14is alkyl, aryl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OH, F, Cl, Br or I; and
R15is an alkyl group.
Yet another embodiment is directed to compounds having formula (IV) including examples 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, and pharmaceutically acceptable salts thereof.
Embodiments of formula (V)
In another aspect, the invention provides a compound of formula (V):
or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3And R5As described herein for formula (I).
In one embodiment of formula (V), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N. In another embodiment of formula (V), X1、X2And X3Is CH. In another embodiment of formula (V), X1And X3Is CH; x2Is N. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1. In another embodiment of formula (V), X2Is CH; x1And X3Is N. In another embodiment of formula (V), X2And X3Is CH; x1Is N.
In another embodiment of formula (V), R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (V), R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), R1Is C (O) NH2. In another embodiment of formula (V), R1Is F. In another embodiment of formula (V), R1Is Cl. In another embodiment of formula (V), R1Is Br. In another embodiment of formula (V), R1Is CN. In another embodiment of formula (V), R1Is NH2. In another embodiment of formula (V), R1Is NO2. In another embodiment of formula (V), R1Is CF3. In another embodiment of formula (V), R1Is C (O) OH.
In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X 1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (V), X1And X3Is CH; x2Is CR1；R1Is C (O) OH.
In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (V), X 2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (V), X 2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (V), X2And X3Is CH; x1Is CR1；R1Is C (O) OH.
In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (V), X1Is CH; x2And X 3Is CR1；R1Is Br. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (V), X1Is CH; x2And X3Is CR1；R1Is C (O) OH.
In one embodiment of formula (V),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N;
R1is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R3is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2OH, F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl, alkenyl and alkynyl group is optionally substituted with one or more groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，C(O)NH2，C(O)OH，OH，CN，CF3F, Cl, Br or I;
R6is an alkyl or heterocyclic group;
R9is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OCH (OCH) 3Or an aryl group;
wherein R is3、R5、R6And R9The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13is alkyl, aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more groups independently selected from: r14，OR14，NH2OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]The pyridyl, pyrrolidin-2-one, cycloalkyl, and cycloalkenyl groups are optionally substituted with one or more groups independently selected from the group consisting of: r15，OR15，C(O)R15，CN，CF3F, Cl, Br or I;
R14is alkyl, aryl or cycloalkyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: OH, F, Cl, Br or I; and
R15is an alkyl group.
Yet another embodiment relates to compounds of formula (V) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 105, 106, 102, 105, 107, 110, 114, 111, 114, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 176, 177, 178, 179, 180, 181, 182, 184, 185, 186, 187, 188, 189, 190, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 209, 210, 211, 213, 214, 215, 216, 217, 218, 219, 220, 221, 223, 224, 225, 226, 227, 228, 230, 231, 232, 234, 235, 236, 237, 239, 240, 243, 245, 246, 248, 249, 250, 251, 252, 253, 254, 256, 257, 258, 259, 260, 265, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 373, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 430, 431, 434, 435, 436, 437, 438, 439, 440, 441, 442, 445, 449, 450, and pharmaceutically acceptable salts thereof.
Embodiments of formula (Ia)
Accordingly, one embodiment of the present invention is directed to compounds useful as inhibitors of NAMPT, or pharmaceutically acceptable salts, the compounds having formula (Ia)
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R2Is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R2The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r4，OR4，SR4，S(O)R4，SO2R4，C(O)R4，CO(O)R4，OC(O)R4，OC(O)OR4，NHC(O)R4，NR4C(O)R4，NHS(O)2R4，NR4S(O)2R4，NHC(O)OR4，NR4C(O)OR4，NHC(O)NH2，NHC(O)NHR4，NHC(O)N(R4)2，NR4C(O)NHR4，NR4C(O)N(R4)2，C(O)NH2，C(O)NHR4，C(O)N(R4)2，C(O)NHOH，C(O)NHOR4，C(O)NHSO2R4，C(O)NR4SO2R4，SO2NH2，SO2NHR4，SO2N(R4)2，C(O)H，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OCH2CH2CH2CH2CH2CH3，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one or more groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein R is2Is other than 4-methylphenyl;
R3is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R 3The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R4is alkyl, alkenyl, alkynyl, aryl, cycloalkyl or heterocyclyl; wherein each R4The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r7，OR7，SR7，S(O)R7，SO2R7，C(O)R7，OC(O)R7，OC(O)OR7，NH2，NHR7，NHC(O)R7，NR7C(O)R7，NHS(O)2R7，NR7S(O)2R7，NHC(O)OR7，NR7C(O)OR7，NHC(O)NH2，NHC(O)NHR7，NHC(O)N(R7)2，NR7C(O)NHR7，NR7C(O)N(R7)2，C(O)NH2，C(O)NHR7，C(O)N(R7)2，C(O)NHOH，C(O)NHOR7，C(O)NHSO2R7，C(O)NR7SO2R7，SO2NH2，SO2NHR7，SO2N(R7)2，C(O)H，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R4The aryl and heterocyclyl groups of (a) are optionally substituted with one or more groups independently selected from: r8，OR8，SR8，S(O)R8，SO2R8，C(O)R8，CO(O)R8，OC(O)R8，OC(O)OR8，NH2，NHR8，NHC(O)R8，NR8C(O)R8，NHS(O)2R8，NR8S(O)2R8，NHC(O)OR8，NR8C(O)OR8，NHC(O)NH2，NHC(O)NHR8，NHC(O)N(R8)2，NR8C(O)NHR8，NR8C(O)N(R8)2，C(O)NH2，C(O)NHR8，C(O)N(R8)2，C(O)NHOH，C(O)NHOR8，C(O)NHSO2R8，C(O)NR8SO2R8，SO2NH2，SO2NHR8，SO2N(R8)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally independently selected by one or moreSubstituted with a group selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R7is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R7The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r11，OR11，SR11，S(O)R11，SO2R11，NHR11，N(R11)2，C(O)R11，C(O)NH2，C(O)NHR11，C(O)N(R11)2，NHC(O)R11，NR11C(O)R11，NHSO2R11，NHC(O)OR11，SO2NH2，SO2NHR11，SO2N(R11)2，NHC(O)NH2，NHC(O)NHR11，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R8Is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R8The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r12，OR12，SR12，S(O)R12，SO2R12，NHR12，N(R12)2，C(O)R12，C(O)NH2，C(O)NHR12，C(O)N(R12)2，NHC(O)R12，NR12C(O)R12，NHSO2R12，NHC(O)OR12，SO2NH2，SO2NHR12，SO2N(R12)2，NHC(O)NH2，NHC(O)NHR12，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3OH, aryl or heterocyclyl;
R10is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R11is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R12is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R 13The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl and cycloalkenyl, optionally substituted with one or more groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from:OCH3，NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3f, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl or cycloalkenyl of (a) is optionally substituted with one or more groups independently selected from: alkyl or OCH3(ii) a And
R15is an alkyl group;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group.
In one embodiment of formula (Ia), X 1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (Ia), X1、X2And X3Is CH. In another embodiment of formula (Ia), X1And X3Is CH; x2Is N. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1. In another embodiment of formula (Ia), X2Is CH; x1And X3Is N. In another embodiment of formula (Ia), X2And X3Is CH; x1Is N. In another embodiment of formula (Ia), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (Ia), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (Ia), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (Ia), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (Ia), R 1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ia), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heteroA cyclic group; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), R1Is C (O) NH2. In another embodiment of formula (Ia), R1Is F. In another embodiment of formula (Ia), R1Is Cl. In another embodiment of formula (Ia), R1Is Br. In another embodiment of formula (Ia), R1Is CN. In another embodiment of formula (Ia), R1Is NH2. In another embodiment of formula (Ia), R1Is NO2. In another embodiment of formula (Ia), R1Is CF3. In another embodiment of formula (Ia), R1Is C (O) OH. In another embodiment of formula (Ia), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (Ia), X1And X3Is CH; x 2Is CR1；R1Is Br. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (Ia), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X 2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (Ia)In scheme (II), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (Ia), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (Ia), X1Is CH; x 2And X3Is CR1；R1Is Br. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (Ia), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In one embodiment of formula (Ia),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N;
R1is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R2is alkyl, phenyl, heterocyclyl, wherein each R is2Is optionally substituted with one or more groups independently selected from: r4，OR4，C(O)R4，CO(O)R4，NHC(O)R4，C(O)NHR4Or F, Cl, Br or I; wherein each R2Optionally substituted at the para position with a group independently selected from: r 5，OCH2CH2CH2CH2CH2CH3，C(O)R5，CO(O)R5，NHR5，NHC(O)R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5，CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl group of (a) is optionally substituted with one or more groups independently selected from: r5，C(O)R5，NHC(O)R5，C(O)NHR5F, Cl, Br or I; wherein R is2Is other than 4-methylphenyl;
R3is alkyl, alkenyl or heterocyclyl; wherein each R3Is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2OH, F, Cl, Br or I;
R4is alkyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Is optionally substituted with one or more groups independently selected from: r7F, Cl, Br or I; wherein each R4The aryl and heterocyclyl groups of (a) are optionally substituted with one or more groups independently selected from: r8，C(O)R8F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl or cycloalkyl; wherein each R5The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，C(O)NH2，C(O)OH，OH，CN，CF3F, Cl, Br or I;
R6is an alkyl or heterocyclic group;
R7is an aryl group;
R8is alkyl, aryl or heterocyclyl;
R9is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R9Is optionally substituted with one or more groups independently selected from: OCH (OCH) 3OH, aryl or heterocyclyl;
wherein R is3、R5、R6、R7、R8And R9The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13，SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13is alkyl, aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furyl, or cycloalkyl; wherein each R13Is optionally substituted with one or more groups independently selected from: r14，OR14，NH2，N(R14)2，NHC(O)R14，OH，CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, and cycloalkyl groups optionally substituted with one or more groups independently selected from: r15，OR15，SO2R15，C(O)R15，N(R15)2，NHC(O)R15，CN，CF3F, Cl, Br or I;
R14Is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R14Is optionally substituted with one or more groups independently selected from: OCH (OCH)3OH, F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl or cycloalkenyl of (a) is optionally substituted with one or more groups independently selected from: alkyl or OCH3(ii) a And
R15is an alkyl group;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group.
In another embodiment of formula (Ia),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N;
R1is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，CN，NH2，NO2，CF3Or C (O) OH;
R2is alkyl, phenyl, heterocyclyl, wherein each R is2Is optionally substituted with one or more groups independently selected from: r4，OR4，C(O)R4，CO(O)R4，NHC(O)R4，C(O)NHR4Or F, Cl, Br or I; wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OCH2CH2CH2CH2CH2CH3，C(O)R5，CO(O)R5，NHR5，NHC(O)R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5Or CF3(ii) a Wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl group of (a) is optionally substituted with one or more groups independently selected from: r5，C(O)R5，NHC(O)R5Or C (O) NHR 5(ii) a Wherein R is2Is other than 4-methylphenyl;
R3is alkyl, alkenyl or heterocyclyl; wherein each R3Is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH;
R4is alkyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Optionally substituted with one or more R7Substitution; wherein each R4The aryl and heterocyclyl groups of (a) are optionally substituted with one or more groups independently selected from: r8，C(O)R8Or Cl;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl or cycloalkyl; wherein each R5The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，C(O)NH2C (O) OH, OH, CN or CF3；
R6Is an alkyl or heterocyclic group;
R7is an aryl group;
R8is alkyl, aryl or heterocyclyl;
R9is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R9Is optionally substituted with one or more groups independently selected from: OCH (OCH)3OH, aryl or heterocyclyl;
wherein R is3、R5、R6、R7、R8And R9The cyclic moiety represented is optionally substituted with one or more groups independently selected fromAnd (3) substitution: r13，OR13，SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F or Cl;
R13is alkyl, aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] ]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furyl, or cycloalkyl; wherein each R13Is optionally substituted with one or more groups independently selected from: r14，OR14，NH2，N(R14)2，NHC(O)R14OH or CF3(ii) a Wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, and cycloalkyl groups optionally substituted with one or more groups independently selected from: r15，OR15，SO2R15，C(O)R15，N(R15)2，NHC(O)R15，CN，CF3F or Cl;
R14is alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R14Is optionally substituted with one or more groups independently selected from: OCH (OCH)3Or OH; wherein each R14The aryl, heterocyclyl, cycloalkyl or cycloalkenyl of (a) is optionally substituted with one or more groups independently selected from: alkyl or OCH 3(ii) a And
R15is an alkyl group;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group.
Yet another embodiment relates to compounds of formula (Ia) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 105, 106, 102, 105, 107, 110, 114, 111, 114, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 358, 359, 360, 361, 362, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 542, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605, 606, 607, 608, 613, 614, 615, 616, 617, 618, 619, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663, 664, 665, 666, 667, 668, 669, 670, 671, 672, 673, 674, 675, 676, 677, 678, 679, 680, 681, 682, 683, 684, 685, 686, 687, 688, 689, 690, 691, 692, 693, 694, 695, 696, 697, 698, 699, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, and pharmaceutically acceptable salts thereof.
Embodiments of the general formula (IIa)
In another aspect, the invention provides a compound of formula (IIa)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3As described herein for formula (Ia); r2Is phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein R is2Phenyl, heterocyclyl, cycloalkyl and cycloalkenyl according to formula (Ia) herein R2The substituents described above are optionally substituted.
In one embodiment of formula (IIa),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R2Is phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OCH2CH2CH2CH2CH2CH3，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one or more groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein R is 2Is other than 4-methylphenyl;
R3is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted by oneOr a plurality of groups independently selected from: OCH (OCH)3OH, aryl or heterocyclyl;
R10is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] ]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloAn alkenyl group; wherein each R13The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl and cycloalkenyl, optionally substituted with one or more groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3，NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R 14The aryl, heterocyclyl, cycloalkyl or cycloalkenyl of (a) is optionally substituted with one or more groups independently selected from: alkyl or OCH3(ii) a And
R15is an alkyl group.
In one embodiment of formula (IIa), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (IIa), X1、X2And X3Is CH. In another embodiment of formula (IIa), X1And X3Is CH; x2Is N. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IIa), X2Is CH; x1And X3Is N. In another embodiment of formula (IIa), X2And X3Is CH; x1Is N. In another embodiment of formula (IIa), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (IIa), X 1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IIa), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (IIa), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IIa), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIa), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), R1Is C (O) NH2. In another embodiment of formula (IIa), R1Is F. In another embodiment of formula (IIa), R1Is Cl. In another embodiment of formula (IIa), R1Is Br. In another embodiment of formula (IIa), R1Is CN. In another embodiment of formula (IIa), R1Is NH2. In another embodiment of formula (IIa), R 1Is NO2. In another embodiment of formula (IIa), R1Is CF3. In another embodiment of formula (IIa), R1Is C (O) OH. In another embodiment of formula (IIa), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X 1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (IIa), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by one or more groups independently selected fromThe following groups are substituted: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X 2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IIa), X 2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IIa), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another of formula (IIa)In an embodiment, X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIa), X 1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IIa), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds of formula (IIa) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 106, 105, 102, 107, 108, 107, 114, 111, 114, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 607, 608, 613, 614, 615, 617, 618, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 682, 683, 684, 685, 686, 687, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, and pharmaceutically acceptable salts thereof.
Embodiments of formula (IIIa)
In another aspect, the invention provides a compound of formula (IIIa)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3As described herein for formula (Ia); when R is2When it is phenyl, RXAs described herein for the substituent in the para position of formula (Ia).
In one embodiment of formula (IIIa),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
RxIs R5，OCH2CH2CH2CH2CH2CH3，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein R isxIs not 4-methyl;
R3is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 6The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3OH, aryl or heterocyclyl;
R10is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R13The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R 13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl and cycloalkenyl, optionally substituted with one or more groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3，NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl or cycloalkenyl of (a) is optionally substituted with one or more groups independently selected from: alkyl or OCH3(ii) a And
R15is an alkyl group.
In one embodiment of formula (IIIa), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x 2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (IIIa), X1、X2And X3Is CH. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is N. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IIIa), X2Is CH; x1And X3Is N. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is N. In another embodiment of formula (IIIa), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (IIIa), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IIIa), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (IIIa), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IIIa), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIa), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), R1Is C (O) NH2. In another embodiment of formula (IIIa), R1Is F. In another embodiment of formula (IIIa), R1Is Cl. In another embodiment of formula (IIIa), R1Is Br. In another embodiment of formula (IIIa), R1Is CN. In another embodiment of formula (IIIa), R1Is NH2. In another embodiment of formula (IIIa), R1Is NO2. In another embodiment of formula (IIIa), R1Is CF3. In another embodiment of formula (IIIa), R1Is C (O) OH. In another embodiment of formula (IIIa), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is R 3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1And X3Is CH; x 2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR 1；R1Is CN. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (HIa), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIa), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more independently Substituted with a group selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X 2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by oneOne or more substituents independently selected from the group consisting of: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIa), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is alkyl or heterocycleAnd (4) a base. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IIIa), X 1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIa), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In one embodiment of formula (IIIa), RxIs R5，OCH2CH2CH2CH2CH2CH3，C(O)R5，CO(O)R5，NHR5，NHC(O)R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5Or CF3(ii) a Wherein R isxIs not 4-methyl. In another embodiment of formula (IIIa), RxIs R5，NHC(O)R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5Or C (O) NHOR5(ii) a Wherein R isxIs not 4-methyl. In another embodiment of formula (IIIa), RxIs R5，R5Is a heterocyclyl group, which is optionally substituted as described in the embodiments herein.
In another embodiment of formula (III), RxIs phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b ][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, pyrrolo [1, 2-d][1，2，4]Triazin-1 (2H) -one, isoindolin-1-one or 1, 2, 3, 6-tetrahydropyridinyl. In another embodiment of formula (III), Rx is phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] o][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, isoindolin-1-keto, or pyrrolo [1, 2-d ]][1，2，4]Triazin-1 (2H) -one; which is optionally substituted as defined herein. In another embodiment of formula (III), Rx is 2, 3, 6-tetrahydropyridinyl; optionally substituted in the manner defined herein.
Yet another embodiment relates to compounds having formula (IIIa) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 101, 105, 100, 106, 102, 107, 110, 114, 111, 114, 111, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 327, 330, 331, 332, 333, 336, 337, 338, 339, 340, 341, 342, 343, 348, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 543, 544, 545, 546, 547, 548, 549, 553, 554, 555, 556, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 607, 608, 613, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 649, 650, 682, 683, 684, 685, 687, 709, 707, 716, 707, 710, and 710.
Yet another embodiment is directed to compounds having formula (IIIa) including examples 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 547, 548, 549, 550, 551, 552, and pharmaceutically acceptable salts thereof.
Embodiments of formula (IVa)
In another aspect, the present invention provides a compound of formula (IVa)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3And R5As described herein for formula (Ia).
In one embodiment of formula (IVa),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Alkyl group of (A) or (B),Alkenyl and alkynyl groups are optionally substituted with one or more groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 5The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3OH, aryl or heterocyclyl;
R10is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally selected by one or more ofSubstituted with a group selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R 13The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl and cycloalkenyl, optionally substituted with one or more groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3，NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl or cycloalkenyl of (a) is optionally substituted with one or more groups independently selected from: alkyl or OCH3(ii) a And
R15is an alkyl group;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group.
In one embodiment of formula (IVa), X 1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (IVa), X1、X2And X3Is CH. In another embodiment of formula (IVa), X1And X3Is CH; x2Is N. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IVa), X2Is CH; x1And X3Is N. In another embodiment of formula (IVa), X2And X3Is CH; x1Is N. In another embodiment of formula (IVa), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (IVa), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IVa), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (IVa), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IVa), R 1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVa), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected fromAnd (3) substitution: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from：R6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), R1Is C (O) NH2. In another embodiment of formula (IVa), R1Is F. In another embodiment of formula (IVa), R1Is Cl. In another embodiment of formula (IVa), R1Is Br. In another embodiment of formula (IVa), R1Is CN. In another embodiment of formula (IVa), R1Is NH2. In another embodiment of formula (IVa), R1Is NO2. In another embodiment of formula (IVa), R1Is CF3. In another embodiment of formula (IVa), R1Is C (O) OH. In another embodiment of formula (IVa), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IVa), X 1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (IVa), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is R 3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IVa), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected fromAnd (3) group substitution: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected fromAnd (3) substitution: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IVa), X 1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IVa), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more independentlySubstituted with a group selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds having formula (IVa), including examples 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 563, 564, 577, 579, 580, 581, 582, 583, 584, 596, 607, 649, 650, 682, 683, 684, 685, and pharmaceutically acceptable salts thereof.
Embodiments of formula (Va)
In another aspect, the invention provides a compound of formula (Va)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3And R5As described herein for formula (Ia).
In one embodiment of formula (Va),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 9The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3OH, aryl or heterocyclyl;
R10is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R13The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl and cycloalkenyl, optionally substituted with one or more groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3，NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl or cycloalkenyl of (a) is optionally substituted with one or more groups independently selected from: alkyl or OCH3(ii) a And
R15is an alkyl group.
In one embodiment of formula (Va), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (Va), X1、X2And X3Is CH. In another embodiment of formula (Va), X1And X3Is CH; x2Is N. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1. In another embodiment of formula (Va), X1Is CH; x2And X 3Is CR1. In another embodiment of formula (Va), X2Is CH; x1And X3Is N. In another embodiment of formula (Va), X2And X3Is CH; x1Is N. In another embodiment of formula (Va), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (Va), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (Va), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (Va), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (Va), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Va), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), R1Is C (O) NH2. In another embodiment of formula (Va), R1Is F. In another embodiment of formula (Va), R 1Is Cl. In another embodiment of formula (Va), R1Is Br. In another embodiment of formula (Va), R1Is CN. In another embodiment of formula (Va), R1Is NH2. In another embodiment of formula (Va), R1Is NO2. In another embodiment of formula (Va), R1Is CF3. In another embodiment of formula (Va), R1Is C (O) OH. In another embodiment of formula (Va), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X 1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (Va), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (Va), X2And X3Is CH; x 1Is CR1；R1Is Br. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is NO2. In another of formula (Va)In one embodiment, X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (Va), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X 1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (Va), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds of formula (Va) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 105, 106, 102, 105, 107, 110, 114, 111, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 373, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 430, 431, 434, 435, 436, 437, 438, 439, 440, 441, 442, 445, 446, 447, 448, 449, 450, 496, 497, 553, 554, 555, 556, 559, 560, 561, 562, 565, 567, 568, 569, 570, 571, 572, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 597, 598, 599, 600, 601, 602, 603, 604, 608, 613, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 686, 687, 716, 717, and pharmaceutically acceptable salts thereof.
Embodiments of formula (VIa)
In another aspect, the present invention provides a compound of formula (VIa)
Or a pharmaceutically acceptable salt thereof; wherein R is1And R5As described herein for formula (Ia); n is 0 or 1.
In one embodiment of formula (VIa),
n is 0 or 1;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3OH, aryl or heterocyclyl;
R10Is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one or more groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R13The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl and cycloalkenyl, optionally substituted with one or more groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more groups independently selected from: OCH (OCH)3，NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl or cycloalkenyl of (a) is optionally substituted with one or more groups independently selected from: alkyl or OCH3(ii) a And
R15is an alkyl group.
In another embodiment of formula (VIa), n is 0. In another embodiment of formula (VIa), n is 1. In another embodiment of formula (VIa), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIa), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIa), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl(ii) a Wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIa), R1Is OR 3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIa), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIa), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIa), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIa), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIa), R 1Is C (O) NH2. In another embodiment of formula (VIa), R1Is F. In another embodiment of formula (VIa), R1Is Cl. In another embodiment of formula (VIa), R1Is Br. In another embodiment of formula (VIa), R1Is CN. In another embodiment of formula (VIa), R1Is NH2. In another embodiment of formula (VIa), R1Is NO2. In another embodiment of formula (VIa), R1Is CF3. In another embodiment of formula (VIa), R1Is C (O) OH. In another embodiment of formula (VIa), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
Yet another embodiment is directed to compounds having formula (VIa) including examples 285, 286, 287, 288, 289, 290, 426, 427, 437, 445, 553, 554, 555, 556, 599, 627, 628, 629, 630, 631, 632, 633, 634, 635, 686, 687, and pharmaceutically acceptable salts thereof.
Embodiments of formula (Ib)
Accordingly, one embodiment of the present invention is directed to compounds useful as inhibitors of NAMPT, or pharmaceutically acceptable salts, the compounds having formula (Ib)
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3，C(O)OH or C (O) NH2；
R2Is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R2Is optionally substituted with one, two, three or four groups independently selected from: r4，OR4，SR4，S(O)R4，SO2R4，C(O)R4，CO(O)R4，OC(O)R4，OC(O)OR4，NHC(O)R4，NR4C(O)R4，NHS(O)2R4，NR4S(O)2R4，NHC(O)OR4，NR4C(O)OR4，NHC(O)NH2，NHC(O)NHR4，NHC(O)N(R4)2，NR4C(O)NHR4，NR4C(O)N(R4)2，C(O)NH2，C(O)NHR4，C(O)N(R4)2，C(O)NHOH，C(O)NHOR4，C(O)NHSO2R4，C(O)NR4SO2R4，SO2NH2，SO2NHR4，SO2N(R4)2，C(O)H，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R3independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r 6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R4independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Is optionally substituted with one, two, three or four groups independently selected from: r7，OR7，SR7，S(O)R7，SO2R7，C(O)R7，OC(O)R7，OC(O)OR7，NH2，NHR7，NHC(O)R7，NR7C(O)R7，NHS(O)2R7，NR7S(O)2R7，NHC(O)OR7，NR7C(O)OR7，NHC(O)NH2，NHC(O)NHR7，NHC(O)N(R7)2，NR7C(O)NHR7，NR7C(O)N(R7)2，C(O)NH2，C(O)NHR7，C(O)N(R7)2，C(O)NHOH，C(O)NHOR7，C(O)NHSO2R7，C(O)NR7SO2R7，SO2NH2，SO2NHR7，SO2N(R7)2，C(O)H，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, C1, Br or I; wherein each R4The aryl and heterocyclyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r8，OR8，SR8，S(O)R8，SO2R8，C(O)R8，CO(O)R8，OC(O)R8，OC(O)OR8，NH2，NHR8，NHC(O)R8，NR8C(O)R8，NHS(O)2R8，NR8S(O)2R8，NHC(O)OR8，NR8C(O)OR8，NHC(O)NH2，NHC(O)NHR8，NHC(O)N(R8)2，NR8C(O)NHR8，NR8C(O)N(R8)2，C(O)NH2，C(O)NHR8，C(O)N(R8)2，C(O)NHOH，C(O)NHOR8，C(O)NHSO2R8，C(O)NR8SO2R8，SO2NH2，SO2NHR8，SO2N(R8)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R7independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkylOr a cycloalkenyl group; wherein each R7Is optionally substituted with one, two, three or four groups independently selected from: r 11，OR11，SR11，S(O)R11，SO2R11，NHR11，N(R11)2，C(O)R11，C(O)NH2，C(O)NHR11，C(O)N(R11)2，NHC(O)R11，NR11C(O)R11，NHSO2R11，NHC(O)OR11，SO2NH2，SO2NHR11，SO2N(R11)2，NHC(O)NH2，NHC(O)NHR11，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R8independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12，SR12，S(O)R12，SO2R12，NHR12，N(R12)2，C(O)R12，C(O)NH2，C(O)NHR12，C(O)N(R12)2，NHC(O)R12，NR12C(O)R12，NHSO2R12，NHC(O)OR12，SO2NH2，SO2NHR12，SO2N(R12)2，NHC(O)NH2，NHC(O)NHR12，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally one, two, three or four independently selected fromThe following groups: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R11independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R12independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R12The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more alkoxy groups;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r 13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furanAnd [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (Ib), X 1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (Ib), X1、X2And X3Is CH. In another embodiment of formula (Ib), X1And X3Is CH; x2Is N. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1. In another embodiment of formula (Ib), X2Is CH; x1And X3Is N. In another embodiment of formula (Ib), X2And X3Is CH; x1Is N. In another embodiment of formula (Ib), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (Ib), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (Ib), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (Ib), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (Ib), R 1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ib), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，C1，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), R1Is C (O) NH2. In another embodiment of formula (Ib), R1Is F. In another embodiment of formula (Ib), R1Is Cl. In another embodiment of formula (Ib), R1Is Br. In another embodiment of formula (Ib), R1Is CN. In another embodiment of formula (Ib), R1Is NH2. In another embodiment of formula (Ib), R1Is NO2. In another embodiment of formula (Ib), R1Is CF3. In another embodiment of formula (Ib), R1Is C (O) OH. In another embodiment of formula (Ib), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (Ib), X1And X3Is CH; x 2Is CR1；R1Is Br. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (Ib), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X 2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (Ib), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (Ib), X1Is CH; x 2And X3Is CR1；R1Is Br. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is CN. In addition to formula (Ib)In one embodiment, X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (Ib), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In one embodiment of formula (Ib), R2Is at para position by R5Substituted phenyl; r5Is phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, pyrrolo [1, 2-d][1，2，4]Triazin-1 (2H) -one or isoindolin-1-one.
In one embodiment of formula (Ib),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R2is alkyl, phenyl, heterocyclyl; wherein each R2Is optionally substituted with one, two, three or four groups independently selected from: r4，OR4，C(O)R4，CO(O)R4NHC(O)R4，NR4C(O)R4，C(O)NHR4Or C (O) N (R)4)2(ii) a Wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OR5，SO2R5，C(O)R5，CO(O)R5，NHR5，NHC(O)R5，NHS(O)2R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5，SO2NHR5，CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl group of (a) is optionally substituted with one, two, three or four groups independently selected from: r5，OR5，C(O)R5，N(R5)2，NHC(O)R5，C(O)NHR5F, Cl, Br or I;
R3at each timeIndependently when present, is selected from alkyl, alkenyl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6OH, F, Cl, Br or I;
R4independently at each occurrence, is selected from alkyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Is optionally substituted with one, two, three or four groups independently selected from: r7F, Cl, Br or I; wherein each R 4The aryl, cycloalkyl and heterocyclyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r8，C(O)R8，CO(O)R8F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，NR9C(O)OR9，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)OH，OH，CN，CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl or heterocyclyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: f, Cl, Br or I;
R7independently at each occurrence, is selected from aryl or heterocyclyl;
R8independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected fromAnd (3) substitution: r12，OR12OH，CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R12Independently at each occurrence, is selected from alkyl, heterocyclyl or cycloalkyl; wherein each R12Optionally substituted with one or more alkoxy groups;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)NHR13，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydro-thiophen-3-yl-1, 1-dioxido-1, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, or cycloalkyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NHC(O)OR14，OH，CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, and cycloalkyl groups optionally substituted with one, two, three, or four groups independently selected from: r 15，OR15，SO2R15，C(O)R15，N(R15)2，NHC(O)R15，CN，CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, OH, F, Cl, Br or I; wherein each R14The aryl, heterocyclyl and cycloalkyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In another embodiment of formula (Ib),
X1、X2and X3Is CH; or
X1And X3Is CH; x 2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R2is alkyl, phenyl, heterocyclyl; wherein each R2Is optionally substituted with one, two, three or four groups independently selected from: r4，OR4，C(O)R4，CO(O)R4NHC(O)R4，NR4C(O)R4，C(O)NHR4Or C (O) N (R)4)2(ii) a Wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OR5，SO2R5，C(O)R5，CO(O)R5，NHR5，NHC(O)R5，NHS(O)2R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5，SO2NHR5Or CF3(ii) a Wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl group of (a) is optionally substituted with one, two, three or four groups independently selected from: r5，OR5，C(O)R5，N(R5)2，NHC(O)R5Or C (O) NHR5；
R3Independently at each occurrence, is selected from alkyl, alkenyl, or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH;
R4independently at each occurrence, is selected from alkyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Optionally with one, two, three or four independently selected R7Substitution; wherein each R4The aryl, cycloalkyl and heterocyclyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r 8，C(O)R8，CO(O)R8F, C1 or Br;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，NR9C(O)OR9，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)OH，OH，CN，CF3Or F;
R6independently at each occurrence, is selected from alkyl or heterocyclyl;
R7independently at each occurrence, is selected from aryl or heterocyclyl;
R8independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12OH or CF3；
R9Independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R12independently at each occurrence, is selected from alkyl, heterocyclyl or cycloalkyl; wherein each R12Optionally substituted with one or more alkoxy groups;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r 13，OR13，SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)NHR13，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F or Cl;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydro-thiophen-3-yl-1, 1-dioxido-1, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, or cycloalkyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NHC(O)OR14OH or CF3(ii) a Wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, and cycloalkyl groups optionally substituted with one, two, three, or four groups independently selected from: r 15，OR15，SO2R15，C(O)R15，N(R15)2，NHC(O)R15，CN，CF3F or Cl;
R14independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy or OH; wherein each R14The aryl, heterocyclyl and cycloalkyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH or Cl;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
Yet another embodiment relates to compounds of formula (Ib) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 105, 106, 102, 107, 108, 107, 114, 111, 114, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 358, 359, 360, 361, 362, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 542, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605, 606, 607, 608, 613, 614, 615, 616, 617, 618, 619, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663, 664, 665, 666, 667, 668, 669, 670, 671, 672, 673, 674, 675, 676, 677, 678, 679, 680, 681, 682, 683, 684, 685, 686, 687, 688, 689, 690, 691, 692, 693, 694, 695, 696, 697, 698, 699, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, 718, 719, 720, 721, 722, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733, 734, 735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 754, 755, 756, 757, 758, 759, 760, 761, 762, 763, 764, 765, 766, 767, 768, 769, 770, 771, 772, 773, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 787, 788, 789, 790, 791, 792, 793, 794, 796, 797, 798, 799, 800, 801, 802, 803, 805, 806, 807, 808, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818, 819, 820, 821, 822, 823, 824, 825, 826, 827, 828, 829, 830, 831, 832, 833, 834, 835, 836, 837, 838, 839, 840, 841, 842, 843, 844, 845, 846, 847, 848, 849, 850, 851, 852, 853, 854, 855, 856, 857, 858, 859, 860, 861, 862, 863, 864, 865, 866, 867, 868, 869, 870, 871, 872, 873, 874, 875, 876, 877, 878, 879, 880, 881, 882, 883, 884, 885, 886, 887, 888, 889, 890, 891, 892, 893, 894, 895, 896, 897, 898, 899, 900, 901, 902, 903, 904, 905, 906, 907, 908, 909, 910, 911, 912, 913, 914, 915, 916, 917, 918, 919, 920, 921, 922, 923, 924, 925, 926, 927, 928, 929, 930, 931, 932, 933, 934, 935, 936, 937, 938, 939, 940, 941, 942, 943, 944, 945, 946, 947, 948, 949, 950, 951, 952, 953, 954, 955, 956, 957, 958, 959, 960, 961, 962, 963, 964, 965, 966, 967, 968, 969, 970, 971, 972, 973, 974, 975, 976, 977, 978, 979, 980, 981, 982, 983, 984, 985, 986, 987, 988, 989, 990, 991, 992, 993, 994, 995, 996, 997, 998, 999, 1000, 1001, 1002, 1003, 1004, 1005, 1006, 1007, 1008, 1009, 1010, 1011, 1012, 1013, 1014, 1015, 1016, 1017, 1018, 1019, 1021, 1022, 1023, 1024, 1025, 1026, 1027, 1028, 1029, 1030, 1031, 1032, 1033, 1034, 1035, 1036, 1037, 1038, 1039, 1040, 1041, 1042, 1043, 1044, 1045, 1046, 1047, 1048, 1049, 1050, 1051, 1052, 1053, 1054, 1055, 1056, 1057, 1058, 1059, 1060, 1061, 1062, 1063, 1064, 1065, 1066, 1067, 1068, 1069, 1070, 1071, 1072, 1073, 1074, 1075, 1076, 1077, 1078, 1079, 1080, 1081, 1082, 1083, 1084, 1085, 1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097, 1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107, 1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, 1121, 1122, 1123, 1124, 1125, 1126, 1127, 1128, 1129, 1130, 1131, 1132, 1133, 1134, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1151, 1152, 1153, 1154, 1155, 1156, 1157, 1158, 1159, 1160, 1161, 1162, 1163, 1164, 1165, 1166, 1167, 1168, 1169, 1170, 1171, 1172, 1173, 1174, 1175, 1176, 1177, 1178, 1179, 1180, 1181, 1182, 1183, 1184, 1185, 1186, 1187, 1188, 1189, 1190, 1191, 1192, 1193, 1194, 1195, 1196, 1197, 1198, 1199, 1200, 1201, 1202, 1203, 1204, 1205, 1206, 1207, 1208, 1209, 1210, 1211, 1212, 1213, 1214, 1215, 1216, 1217, 1218, 1219, 1220, 1221, 1222, 1223, 1224, 1225, 1226, 1227, 1228, 1229, 1230, 1231, 1232, 1233, 1234, 1235, 1236, 1237, 1238, 1239, 1240, 1241, 1242, 1243, 1244, 1245, 1246, 1247, 1248, 1249, 1250, 1251, 1252, 1253, 1254, 1255, 1256, 1257, 1258, 1259, 1260, 1261, 1262, 1263, 1264, 1265, 1266, 1267, 1269, 1270, 1271, 1272, 1273, 1274, 1275, 1276, 1277, 1278, 1279, 1280, 1281, 1282, 1283, 1284, 1285, 1286, 1287, 1288, 1289, 1292, 1293, 1294, 1295, 1296, 1297, 1298, 1299, 1300, 1301, 1302, 1303, 1304, 1305, 1306, 1307, 1308, 1309, 1310, 1311, 1312, 1313, 1314, 1315, 1316, 1317, 1318, 1319, 1320, 1321, 1322, 1323, 1324, 1325, 1326, 1327, 1328, 1329, 1330, 1331, 1332, 1333, 1334, 1335, 1336, 1337, 1338, 1339, 1340, 1341, 1342, 1343, 1344, 1345, 1346, 1347, 1348, 1349, 1350, 1351, 1352, 1353, 1354, 1355, 1356, 1357, 1358, 1359, 1360, 1361, 1362, 1363, 1364, 1365, 1366, 1367, 1368, 1369, 1370, 1371, 1372, 1373, 1374, 1375, 1376, 1377, 1378, 1379, 1380, 1381, 1382, 1383, 1384, 1385, 1386, 1387, 1388, 1389, 1390, 1391, 1392, 1393, 1394, 1395, 1396, 1397, 1398, 1399, 1400, 1401, 1402, 1403, 1404, 1405, 1406, 1407, 1408, 1409, 1410, 1411, 1412, 1413, 1414, 1415, 1416, 1417, 1418, 1419, 1420, 1421, 1422, 1423, 1424, 1425, 1426, or a pharmaceutically acceptable salt thereof.
Embodiments of formula (IIb)
In another aspect, the present invention provides compounds of formula (IIb)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3As described herein for formula (Ib); r2Is phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein R is2Phenyl, heterocyclyl, cycloalkyl and cycloalkenyl according to formula (Ib) herein R2The substituents described above are optionally substituted.
In one embodiment of formula (IIb),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R2Is phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R2Optionally substituted at the para position with one group independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
Wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected fromGroup substitution: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (IIb), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x 2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (IIb), X1、X2And X3Is CH. In another embodiment of formula (IIb), X1And X3Is CH; x2Is N. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IIb), X2Is CH; x1And X3Is N. In another embodiment of formula (IIb), X2And X3Is CH; x1Is N. In another embodiment of formula (IIb), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (IIb), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IIb), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (IIb), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IIb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIb), R 1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl;wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is 6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), R1Is C (O) NH2. In another embodiment of formula (IIb), R1Is F. In another embodiment of formula (IIb), R1Is Cl. In another embodiment of formula (IIb), R1Is Br. In another embodiment of formula (IIb), R1Is CN. In another embodiment of formula (IIb), R1Is NH2. In another embodiment of formula (IIb), R1Is NO2. In another embodiment of formula (IIb), R1Is CF3. In another embodiment of formula (IIb), R1Is C (O) OH. In another embodiment of formula (IIb), R1Is C (O) R3(ii) a Wherein R is3Is an alkyl groupAlkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIb)In, X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IIb), X 1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IIb), X1And X3Is CH; x2Is C R1；R1Is C (O) OH. In another embodiment of formula (IIb), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is R 3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by one or more groups independently selected fromThe following groups: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IIb)In, X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IIb), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl(ii) a Wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IIb), X 1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IIb), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds of formula (IIb) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 101, 105, 100, 106, 102, 107, 110, 114, 111, 114, 111, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 607, 608, 613, 614, 615, 617, 618, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 682, 683, 684, 685, 686, 687, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, 718, 719, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733, 734, 735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 754, 755, 756, 758, 759, 760, 761, 762, 763, 764, 765, 766, 767, 768, 769, 770, 771, 772, 773, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 787, 788, 789, 790, 791, 792, 793, 794, 796, 799, 800, 801, 802, 803, 805, 806, 808, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818, 819, 820, 821, 822, 823, 824, 825, 826, 827, 828, 829, 830, 831, 832, 833, 834, 835, 836, 837, 838, 839, 840, 841, 842, 843, 844, 845, 846, 847, 848, 849, 850, 851, 852, 853, 854, 855, 856, 857, 858, 859, 860, 861, 862, 863, 864, 865, 866, 867, 868, 869, 870, 871, 873, 874, 875, 876, 877, 878, 879, 880, 881, 882, 883, 884, 885, 886, 887, 888, 889, 890, 891, 892, 893, 894, 895, 896, 897, 898, 899, 900, 901, 902, 903, 904, 905, 906, 907, 908, 910, 911, 912, 913, 914, 915, 916, 917, 918, 919, 920, 922, 923, 924, 925, 926, 927, 928, 929, 930, 931, 932, 933, 934, 935, 936, 937, 938, 939, 940, 941, 942, 943, 944, 945, 946, 947, 948, 949, 950, 951, 952, 953, 954, 955, 956, 957, 958, 959, 960, 961, 962, 963, 964, 965, 966, 967, 968, 969, 970, 971, 972, 973, 974, 975, 976, 977, 978, 979, 980, 981, 982, 983, 984, 985, 986, 987, 988, 989, 990, 991, 992, 993, 994, 995, 996, 997, 998, 999, 1000, 1001, 1002, 1003, 1004, 1005, 1006, 1007, 1008, 1009, 1010, 1011, 1012, 1013, 1014, 1015, 1016, 1017, 1018, 1019, 1021, 1022, 1023, 1024, 1025, 1026, 1027, 1028, 1029, 1030, 1031, 1032, 1033, 1034, 1035, 1036, 1037, 1038, 1039, 1040, 1041, 1042, 1043, 1044, 1045, 1046, 1047, 1048, 1049, 1050, 1051, 1052, 1053, 1054, 1055, 1056, 1057, 1058, 1059, 1060, 1061, 1062, 1063, 1064, 1065, 1066, 1067, 1068, 1069, 1070, 1071, 1072, 1073, 1074, 1075, 1076, 1077, 1078, 1079, 1080, 1081, 1082, 1083, 1084, 1085, 1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097, 1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107, 1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, 1121, 1122, 1123, 1124, 1125, 1126, 1127, 1128, 1129, 1130, 1131, 1132, 1133, 1134, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1151, 1152, 1153, 1154, 1155, 1156, 1157, 1158, 1159, 1160, 1161, 1162, 1163, 1164, 1165, 1166, 1167, 1168, 1169, 1170, 1171, 1172, 1173, 1174, 1175, 1176, 1177, 1178, 1179, 1180, 1181, 1182, 1183, 1184, 1185, 1186, 1187, 1188, 1189, 1190, 1191, 1192, 1193, 1194, 1195, 1196, 1197, 1198, 1199, 1200, 1201, 1202, 1203, 1204, 1205, 1206, 1207, 1208, 1209, 1210, 1211, 1212, 1213, 1214, 1215, 1216, 1217, 1218, 1219, 1220, 1221, 1222, 1223, 1224, 1225, 1226, 1227, 1228, 1229, 1230, 1231, 1232, 1233, 1234, 1235, 1236, 1237, 1238, 1239, 1240, 1241, 1242, 1243, 1244, 1245, 1246, 1247, 1248, 1249, 1250, 1251, 1252, 1253, 1254, 1255, 1256, 1257, 1258, 1259, 1260, 1261, 1262, 1263, 1264, 1265, 1266, 1267, 1269, 1270, 1271, 1272, 1273, 1274, 1275, 1276, 1277, 1278, 1279, 1280, 1281, 1282, 1283, 1284, 1288, 1289, 1292, 1293, 1294, 1295, 1296, 1297, 1298, 1299, 1300, 1301, 1302, 1303, 1304, 1305, 1306, 1307, 1308, 1309, 1310, 1311, 1312, 1313, 1314, 1315, 1316, 1317, 1318, 1319, 1320, 1321, 1322, 1323, 1324, 1325, 1326, 1327, 1328, 1329, 1330, 1331, 1332, 1333, 1334, 1335, 1336, 1337, 1338, 1339, 1340, 1341, 1342, 1343, 1344, 1345, 1346, 1347, 1348, 1349, 1363, 1364, 1365, 1366, 1367, 1368, 1370, 1371, 1372, 1373, 1374, 1375, 1376, 1377, 1378, 1379, 1380, 1381, 1382, 1383, 1384, 1385, 1386, 1387, 1388, 1389, 1390, 1391, 1392, 1393, 1394, 1395, 1396, 1397, 1398, 1399, 1400, 1401, 1402, 1403, 1404, 1405, 1406, 1407, 1408, 1409, 1410, 1411, 1412, 1413, 1414, 1415, 1416, 1417, 1418, 1419, 1420, 1421, 1422, 1423, 1424, 1425, 1426, or a pharmaceutically acceptable salt thereof.
Embodiments of formula (IIIb)
In another aspect, the invention provides a compound of formula (IIIb)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3As described herein for formula (Ib); when R is2When it is phenyl, RXAs described herein for the substituent in the para position of formula (Ib).
In one embodiment of formula (IIIb),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
Rx is R5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I;
R3independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r 9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from alkylAlkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl or cycloalkenyl; wherein each R 13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyranylPyrrolyl, thienyl, furyl, morpholinyl, cycloalkyl and cycloalkenyl are optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r 16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when X is1、X2And X3When is CH, RxIs not methyl;
provided that when X is1、X2And X3When is CH, RxIs not methoxy;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (IIIb), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (IIIb), X1、X2And X3Is CH. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is N. In another embodiment of formula (IIIb),X1and X3Is CH; x2Is CR1. In another embodiment of formula (IIIb), X2And X 3Is CH; x1Is CR1. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IIIb), X2Is CH; x1And X3Is N. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is N. In another embodiment of formula (IIIb), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (IIIb), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IIIb), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (IIIb), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IIIb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; it is composed ofWherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), R 1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is 6Is alkyl or heterocyclyl. In another embodiment of formula (IIIb), R1Is C (O) NH2. In another embodiment of formula (IIIb), R1Is F. In another embodiment of formula (IIIb), R1Is Cl. In another embodiment of formula (IIIb), R1Is Br. In another embodiment of formula (IIIb), R1Is CN. In another embodiment of formula (IIIb), R1Is NH2. In another embodiment of formula (IIIb), R1Is NO2. In another embodiment of formula (IIIb), R1Is CF3. In another embodiment of formula (IIIb), R1Is C (O) OH. In another embodiment of formula (IIIb), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is 6Is alkyl or heterocyclyl. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X 1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is CF 3. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by one or moreEach independently selected from the group consisting of: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X 2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is 3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IIIb), X1Is CH; x2And X 3Is CR1；R1Is NO2. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In one embodiment of formula (IIIb), RxIs R5，OR5，SO2R5，C(O)R5，CO(O)R5，NHR5，NHC(O)R5，NHS(O)2R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5，SO2NHR5Or CF3. In another embodiment of formula (IIIb), RxIs R5，R5Is a heterocyclyl group, which is optionally substituted as described in the embodiments herein.
In another embodiment of formula (IIIb), RxIs phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, pyrrolo [1, 2-d][1，2，4]Triazin-1 (2H) -one, isoindolin-1-one or 1, 2, 3, 6-tetrahydropyridinyl. In another embodiment of formula (IIIb), RxIs phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b ][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, isoindolin-1-keto, or pyrrolo [1, 2-d ]][1，2，4]Triazin-1 (2H) -one; which is optionally substituted as defined herein. In another embodiment of formula (IIIb), RxIs, 2, 3, 6-tetrahydropyridinyl; which is optionally substituted as defined herein.
Yet another embodiment relates to compounds having formula (IIIb) including examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 101, 105, 100, 106, 102, 107, 110, 114, 111, 114, 111, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 327, 330, 331, 332, 333, 336, 337, 338, 339, 340, 341, 342, 343, 348, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 543, 544, 545, 546, 547, 548, 549, 553, 554, 555, 556, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 607, 608, 613, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 649, 650, 682, 683, 684, 685, 686, 687, 705, 706, 707, 708, 709, 710, 716, 717, 718, 719, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733, 734, 735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 754, 755, 756, 759, 760, 761, 762, 763, 770, 771, 772, 773, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 787, 788, 789, 790, 791, 792, 793, 794, 796, 799, 802, 803, 806, 808, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818, 819, 820, 821, 822, 823, 824, 825, 826, 827, 828, 829, 830, 831, 832, 833, 834, 835, 836, 837, 838, 840, 841, 842, 843, 844, 845, 846, 847, 848, 849, 850, 851, 852, 853, 854, 855, 856, 857, 858, 859, 860, 861, 862, 863, 864, 865, 866, 867, 868, 869, 870, 871, 873, 874, 875, 876, 877, 878, 879, 880, 881, 882, 883, 884, 885, 886, 887, 888, 889, 890, 891, 892, 893, 894, 895, 896, 897, 898, 899, 900, 901, 902, 903, 904, 905, 906, 907, 908, 910, 911, 912, 913, 914, 915, 916, 917, 918, 919, 922, 923, 924, 925, 926, 927, 928, 929, 930, 931, 932, 933, 934, 935, 936, 937, 938, 939, 940, 941, 942, 943, 944, 945, 946, 947, 948, 949, 950, 951, 952, 966, 967, 968, 969, 970, 971, 972, 973, 974, 975, 976, 977, 978, 979, 980, 981, 982, 983, 984, 985, 986, 987, 988, 989, 990, 991, 992, 993, 994, 995, 996, 997, 998, 999, 1000, 1001, 1002, 1003, 1004, 1005, 1006, 1007, 1008, 1009, 1010, 1011, 1012, 1013, 1014, 1015, 1016, 1017, 1018, 1019, 1021, 1022, 1023, 1024, 1025, 1026, 1027, 1028, 1029, 1030, 1031, 1032, 1033, 1034, 1035, 1036, 1037, 1038, 1039, 1040, 1041, 1042, 1043, 1044, 1045, 1046, 1047, 1048, 1049, 1050, 1051, 1052, 1053, 1054, 1055, 1056, 1057, 1058, 1059, 1060, 1061, 1062, 1063, 1064, 1065, 1066, 1067, 1068, 1069, 1070, 1071, 1072, 1073, 1074, 1075, 1076, 1077, 1078, 1079, 1080, 1081, 1082, 1083, 1084, 1085, 1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097, 1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107, 1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, 1121, 1122, 1123, 1124, 1125, 1126, 1127, 1128, 1129, 1130, 1131, 1132, 1133, 1134, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1151, 1152, 1153, 1154, 1155, 1156, 1157, 1158, 1159, 1160, 1161, 1162, 1163, 1164, 1165, 1166, 1167, 1168, 1169, 1170, 1171, 1172, 1173, 1174, 1175, 1176, 1177, 1178, 1179, 1180, 1181, 1182, 1183, 1184, 1185, 1186, 1187, 1188, 1189, 1190, 1191, 1192, 1193, 1194, 1195, 1196, 1197, 1198, 1199, 1200, 1201, 1202, 1203, 1204, 1205, 1206, 1207, 1208, 1209, 1210, 1211, 1212, 1213, 1214, 1215, 1216, 1217, 1218, 1219, 1220, 1221, 1222, 1223, 1224, 1225, 1226, 1227, 1228, 1229, 1230, 1231, 1232, 1233, 1234, 1235, 1236, 1237, 1238, 1239, 1240, 1241, 1242, 1243, 1244, 1245, 1246, 1247, 1248, 1249, 1250, 1251, 1252, 1253, 1254, 1255, 1256, 1257, 1258, 1259, 1260, 1261, 1262, 1263, 1264, 1265, 1266, 1267, 1269, 1270, 1271, 1272, 1273, 1274, 1275, 1276, 1277, 1278, 1279, 1280, 1281, 1282, 1283, 1284, 1288, 1289, 1292, 1293, 1294, 1295, 1296, 1297, 1298, 1299, 1300, 1301, 1302, 1303, 1304, 1305, 1306, 1307, 1308, 1309, 1310, 1311, 1312, 1313, 1314, 1315, 1316, 1317, 1318, 1319, 1320, 1321, 1322, 1323, 1324, 1325, 1326, 1327, 1328, 1329, 1330, 1331, 1332, 1333, 1334, 1335, 1336, 1337, 1338, 1339, 1340, 1341, 1342, 1343, 1344, 1345, 1346, 1347, 1348, 1349, 1363, 1364, 1365, 1336, 1367, 1368, 1370, 1371, 1372, 1373, 1374, 1375, 1376, 1377, 1378, 1379, 1380, 1381, 1382, 1383, 1424, 1385, 1386, 1387, 1388, 1389, 1390, 1391, 1392, 1393, 1395, 1396, 1397, 1398, 1399, 1395, 1423, 1415, 1421, 1415, 1405 3, 1414, 1423, 1415, 1414, 1423, 1405, 1414, 1415, 1414, 1421, 1415, and 1414, 1414.
Yet another embodiment relates to compounds having formula (IIIb) including 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 547, 548, 549, 550, 551, 552, and pharmaceutically acceptable salts thereof.
Embodiments of formula (IVb)
In another aspect, the invention provides a compound of formula (IVb)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3And R5As described herein for formula (Ib).
In one embodiment of formula (IVb),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted by one, two, three, four, five orSix groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] ]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (IVb), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (IVb), X1、X2And X 3Is CH. In another embodiment of formula (IVb), X1And X3Is CH; x2Is N. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IVb), X2Is CH; x1And X3Is N. In another embodiment of formula (IVb), X2And X3Is CH; x1Is N. In another embodiment of formula (IVb), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (IVb), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IVb), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (IVb), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IVb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocycleA group; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), R1Is C (O) NH2. In another embodiment of formula (IVb), R1Is F. In another embodiment of formula (IVb), R1Is Cl. In another embodiment of formula (IVb), R1Is Br. In another embodiment of formula (IVb), R1Is CN. In another embodiment of formula (IVb), R1Is NH2. In another embodiment of formula (IVb), R1Is NO2. In another embodiment of formula (IVb), R1Is CF3. In another embodiment of formula (IVb), R1Is C (O) OH. In another embodiment of formula (IVb), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is 6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by oneOne or more substituents independently selected from the group consisting of: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1And X 3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IVb), X 1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (IVb), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is an alkyl group,An alkenyl or heterocyclyl group; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X 2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IVb), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more independentlySubstituted with a group selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X 1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IVb), X 1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IVb), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds having formula (IVb), including examples 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 563, 564, 577, 579, 580, 581, 582, 583, 584, 596, 607, 649, 650, 682, 683, 684, 685, 789, 791, 792, 793, 794, 796, 874, 878, 879, 919, 932, 934, 935, 1363, 1364, 1365, 1366, 1367, 1368, 1370, 1371, 1372, or pharmaceutically acceptable salts thereof.
Embodiments of formula (Vb)
In another aspect, the present invention provides a compound of formula (Vb)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3And R5As described herein for formula (Ib).
In one embodiment of formula (Vb),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x 1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each one ofR is6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R 13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，F，Cl，Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is 16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (Vb), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (Vb), X1、X2And X3Is CH. In another embodiment of formula (Vb), X1And X3Is CH; x2Is N. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1. In another embodiment of formula (Vb), X2Is CH; x1And X3Is N. In another embodiment of formula (Vb), X2And X3Is CH; x1Is N. In another embodiment of formula (Vb), X 1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (Vb), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (Vb), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (Vb), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (Vb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Vb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), R1Is C (O) NH2. In another embodiment of formula (Vb), R1Is F. In another embodiment of formula (Vb), R1Is Cl. In another embodiment of formula (Vb), R1Is Br. In another embodiment of formula (Vb), R1Is CN. In another embodiment of formula (Vb), R1Is NH2. In another embodiment of formula (Vb), R 1Is NO2. In another embodiment of formula (Vb), R1Is CF3. In another embodiment of formula (Vb), R1Is C (O) OH. In another embodiment of formula (Vb), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X 1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (Vb), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is alkyl or heterocyclyl. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X 2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (Vb), X 2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (Vb), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is 6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vb), X 1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (Vb), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds of formula (Vb) including examples 1, 2, 3, 4, 5, 8, 9, 10, 13, 14, 16, 17, 18, 20, 21, 23, 24, 25, 26, 28, 29, 30, 31, 32, 33, 34, 36, 37, 38, 39, 40, 42, 43, 45, 46, 48, 49, 53, 54, 57, 58, 59, 60, 61, 62, 63, 66, 67, 68, 70, 71, 73, 75, 77, 79, 80, 81, 82, 83, 85, 86, 87, 88, 90, 91, 92, 93, 94, 95, 97, 98, 99, 100, 101, 103, 104, 105, 106, 107, 108, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 131, 129, 130, 135, 141, 143, 142, 145, 142, 145, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 159, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 176, 177, 178, 179, 180, 181, 182, 184, 188, 189, 190, 192, 193, 194, 196, 199, 201, 203, 204, 205, 209, 210, 211, 213, 215, 217, 220, 223, 224, 226, 227, 228, 230, 231, 232, 234, 235, 236, 237, 239, 243, 245, 252, 253, 256, 258, 260, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 288, 289, 290, 373, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 426, 427, 430, 431, 435, 436, 437, 440, 441, 442, 445, 446, 447, 449, 450, 496, 497, 553, 554, 555, 556, 559, 560, 562, 567, 568, 569, 570, 571, 572, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 597, 598, 599, 600, 601, 602, 603, 604, 608, 613, 625, 626, 628, 629, 630, 631, 632, 633, 634, 687, 716, 717, 718, 719, 723, 728, 729, 731, 732, 733, 734, 735, 737, 738, 739, 741, 743, 744, 745, 747, 748, 752, 770, 771, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 790, 802, 803, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818, 819, 820, 821, 822, 823, 826, 827, 829, 830, 831, 832, 833, 834, 835, 836, 837, 838, 856, 857, 858, 875, 880, 881, 882, 884, 894, 895, 922, 923, 924, 925, 939, 969, 970, 971, 972, 976, 977, 978, 1063, 1064, 1065, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097, 1098, 1100, 1102, 1103, 1104, 1105, 1106, 1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, 1121, 1122, 1123, 1124, 1125, 1127, 1129, 1130, 1132, 1133, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1152, 1153, 1154, 1155, 1156, 1157, 1158, 1160, 1161, 1162, 1163, 1164, 1165, 1166, 1167, 1168, 1169, 1170, 1171, 1172, 1173, 1174, 1175, 1176, 1177, 1178, 1179, 1180, 1181, 1182, 1183, 1184, 1185, 1186, 1187, 1188, 1189, 1192, 1193, 1194, 1195, 1196, 1197, 1198, 1199, 1201, 1202, 1203, 1204, 1205, 1206, 1207, 1208, 1209, 1210, 1211, 1212, 1213, 1214, 1215, 1216, 1217, 1218, 1219, 1220, 1221, 1222, 1223, 1224, 1225, 1226, 1227, 1228, 1229, 1230, 1231, 1232, 1233, 1234, 1235, 1236, 1239, 1240, 1241, 1242, 1243, 1245, 1260, 1261, 1262, 1263, 1264, 1266, 1267, 1268, 1269, 1270, 1271, 1272, 1273, 1274, 1275, 1276, 1277, 1278, 1310, 1311, 1312, 1313, 1314, 1315, 1316, 7, 1318, 1319, 1320, 1321, 1322, 1323, 1324, 1325, 1326, 1327, 1328, 1329, 1330, 1331, 1332, 1333, 1334, 1335, 1336, 1327, 1338, 1339, 1340, 1341, 1342, 1343, 1344, 1345, 1346, 1348, 1349, or a pharmaceutically acceptable salt thereof.
Embodiments of formula (VIb)
In another aspect, the present invention provides a compound of formula (VIb)
Or a pharmaceutically acceptable salt thereof; wherein R is1And R5As described herein for formula (Ia); n is 0 or 1.
In one embodiment of formula (VIb),
n is 0 or 1;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranPyridyl, pyridazinyl, pyrazinyl, pyrimidinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R 13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothien-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinylCycloalkyl and cycloalkenyl are optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is 16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl.
In another embodiment of formula (VIb), n is 0. In another embodiment of formula (VIb), n is 1. In another embodiment of formula (VIb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，B r，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIb), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIb), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from:R6，OR6，NH2，NHC(O)R6，N(R6)2or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIb), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIb), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIb), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIb), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIb), R1Is C (O) NH2. In another embodiment of formula (VIb), R1Is F. In another embodiment of formula (VIb), R1Is Cl. In another embodiment of formula (VIb), R1Is Br. In another embodiment of formula (VIb), R1Is CN. In another embodiment of formula (VIb), R1Is NH2. In another embodiment of formula (VIb) ，R1Is NO2. In another embodiment of formula (VIb), R1Is CF3. In another embodiment of formula (VIb), R1Is C (O) OH. In another embodiment of formula (VIb), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds having formula (VIb) including pharmaceutically acceptable salts such as, for example 285, 286, 288, 289, 290, 426, 427, 437, 445, 553, 554, 555, 556, 599, 627, 628, 629, 630, 631, 632, 633, 634, 635, 686, 687, 718, 723, 725, 726, 727, 728, 729, 731, 732, 733, 734, 735, 737, 738, 739, 741, 748, 744, 745, 747, 881, 770, 771, 773, 774, 775, 776, 777, 778, 779, 780, 803, 875, 880, 881, 882, 884, 922, 923, 924, 925, 939, 969, 970, 971, 972, 1055, 1056, 1057, 1058, 1059, 1061, 1062, 1063, 1074, 1075, 1065, 1066, 1064, 1065, 1063, 1065, 1062, 1065, 1066, 1062, 1065, 1063, 1062, 1065, 1062, 1065, or 1062.
An embodiment of the formula (VIIb)
In another aspect, the present invention provides a compound of formula (VIIb)
Or a pharmaceutically acceptable salt thereof; wherein X1、X2、X3And R13As described herein for formula (Ib),represents a single or double bond.
In one embodiment of formula (VIIb),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each one ofR is6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
Wherein R is3、R6And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl, 1-tetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (VIIb), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x 3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (VIIb), X1、X2And X3Is CH. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is N. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1. In another embodiment of formula (VIIb), X2Is CH; x1And X3Is N. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is N. In another embodiment of formula (VIIb), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (VIIb), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (VIIb), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (VIIb), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (VIIb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIb), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), R1Is C (O) NH2. In another embodiment of formula (VIIb), R1Is F. In another embodiment of formula (VIIb), R1Is Cl. In another embodiment of formula (VIIb), R1Is Br. In another embodiment of formula (VIIb), R1Is CN. In another embodiment of formula (VIIb), R1Is NH2. In another embodiment of formula (VIIb), R1Is NO2. In another embodiment of formula (VIIb), R1Is CF3. In another embodiment of formula (VIIb), R1Is C (O) OH. In another embodiment of formula (VIIb), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is R 3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1And X3Is CH; x 2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by oneOne or more substituents independently selected from the group consisting of: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR 1；R1Is CN. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIb), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a It is composed ofIn R3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X 2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In-situ type(VIIb) another embodiment of X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIb), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkaneOptionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (VIIb), X 1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIb), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds having formula (VIIb) including, for example 317, 330, 331, 332, 401, 405, 406, 407, 432, 456, 457, 458, 459, 460, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 543, 544, 545, 546, 620, 646, 647, 705, 706, 707, 708, 709, 710, 759, 760, 761, 762, 763, 799, 910, 911, 912, 913, 914, 915, 916, 917, 918, 967, 968, 979, 980, 981, 982, 983, 984, 985, 986, 1015, 1077, 1011077, 1077, 1011079, 1257, 1254, 1255, 1254, 1282, 1254, 1289, 1287, 1282, 1287, 1254, 1259, 1254, 128.
Embodiments of formula (Ic)
Accordingly, one embodiment of the present invention is directed to compounds useful as inhibitors of NAMPT, or pharmaceutically acceptable salts, the compounds having formula (Ic)
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R2Is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R2Is optionally substituted with one, two, three or four groups independently selected from: r4，OR4，SR4，S(O)R4，SO2R4，C(O)R4，CO(O)R4，OC(O)R4，OC(O)OR4，NHC(O)R4，NR4C(O)R4，NHS(O)2R4，NR4S(O)2R4，NHC(O)OR4，NR4C(O)OR4，NHC(O)NH2，NHC(O)NHR4，NHC(O)N(R4)2，NR4C(O)NHR4，NR4C(O)N(R4)2，C(O)NH2，C(O)NHR4，C(O)N(R4)2，C(O)NHOH，C(O)NHOR4，C(O)NHSO2R4，C(O)NR4SO2R4，SO2NH2，SO2NHR4，SO2N(R4)2，C(O)H，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R3independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R 3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R4independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Is optionally substituted with one, two, three or four groups independently selected from: r7，OR7，SR7，S(O)R7，SO2R7，C(O)R7，OC(O)R7，OC(O)OR7，NH2，NHR7，NHC(O)R7，NR7C(O)R7，NHS(O)2R7，NR7S(O)2R7，NHC(O)OR7，NR7C(O)OR7，NHC(O)NH2，NHC(O)NHR7，NHC(O)N(R7)2，NR7C(O)NHR7，NR7C(O)N(R7)2，C(O)NH2，C(O)NHR7，C(O)N(R7)2，C(O)NHOH，C(O)NHOR7，C(O)NHSO2R7，C(O)NR7SO2R7，SO2NH2，SO2NHR7，SO2N(R7)2，C(O)H，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R4The aryl and heterocyclyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r8，OR8，SR8，S(O)R8，SO2R8，C(O)R8，CO(O)R8，OC(O)R8，OC(O)OR8，NH2，NHR8，NHC(O)R8，NR8C(O)R8，NHS(O)2R8，NR8S(O)2R8，NHC(O)OR8，NR8C(O)OR8，NHC(O)NH2，NHC(O)NHR8，NHC(O)N(R8)2，NR8C(O)NHR8，NR8C(O)N(R8)2，C(O)NH2，C(O)NHR8，C(O)N(R8)2，C(O)NHOH，C(O)NHOR8，C(O)NHSO2R8，C(O)NR8SO2R8，SO2NH2，SO2NHR8，SO2N(R8)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5at each time of dischargeWhen present, is independently selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R7independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 7Is optionally substituted with one, two, three or four groups independently selected from: r11，OR11，SR11，S(O)R11，SO2R11，NHR11，N(R11)2，C(O)R11，C(O)NH2，C(O)NHR11，C(O)N(R11)2，NHC(O)R11，NR11C(O)R11，NHSO2R11，NHC(O)OR11，SO2NH2，SO2NHR11，SO2N(R11)2，NHC(O)NH2，NHC(O)NHR11，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R8independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12，SR12，S(O)R12，SO2R12，NHR12，N(R12)2，C(O)R12，C(O)NH2，C(O)NHR12，C(O)N(R12)2，NHC(O)R12，NR12C(O)R12，NHSO2R12，NHC(O)OR12，SO2NH2，SO2NHR12，SO2N(R12)2，NHC(O)NH2，NHC(O)NHR12，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R11independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R12independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R12The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more alkoxy groups;
Wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from the group consisting of alkanesA group, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I; wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
R15independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted with one, two, three or four alkoxy groups;
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group;
provided that when R is 13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (Ic), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (Ic), X1、X2And X3Is CH. In another embodiment of formula (Ic), X1And X3Is CH; x2Is N. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1. In another embodiment of formula (Ic), X2Is CH; x1And X3Is N. In another embodiment of formula (Ic), X2And X3Is CH; x1Is N. In another embodiment of formula (Ic), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (Ic), X1Is CR1；X2Is N; x 3Is CH. In another embodiment of formula (Ic), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (Ic), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (Ic), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ic), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic)，R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), R1Is C (O) NH2. In another embodiment of formula (Ic), R1Is F. In another embodiment of formula (Ic), R1Is Cl. In another embodiment of formula (Ic), R1Is Br. In another embodiment of formula (Ic), R1Is CN. In another embodiment of formula (Ic), R1Is NH2. In another embodiment of formula (Ic), R 1Is NO2. In another embodiment of formula (Ic), R1Is CF3. In another embodiment of formula (Ic), R1Is C (O) OH. In another embodiment of formula (Ic), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X 1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (Ic), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted Substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X 2And X3Is CH; x1Is CR1；R1Is NHC(O)R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (Ic), X 2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (Ic), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each one ofOptionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is 6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Ic), X 1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (Ic), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In one embodiment of formula (Ic), R2Is at para position by R5Substituted phenyl; r5Is phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b ][1，2]Diaza derivatives-a 4(5H) -keto group,5- (trifluoromethyl) phthalazin-1 (2H) -one, pyrrolo [1, 2-d][1，2，4]Triazin-1 (2H) -one or isoindolin-1-one.
In one embodiment of formula (Ic),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R2is alkyl, phenyl, cycloalkyl or heterocyclyl; wherein each R2Is optionally substituted with one, two, three or four groups independently selected from: r4，OR4，C(O)R4，CO(O)R4NHC(O)R4，NR4C(O)R4，C(O)NHR4Or C (O) N (R)4)2(ii) a Wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OR5，SO2R5，C(O)R5，CO(O)R5，NHR5，NHC(O)R5，NHS(O)2R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5，SO2NHR5，CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl and cycloalkyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r5，OR5，C(O)R5，C(O)OR5，N(R5)2，NHC(O)R5，C(O)NHR5F, Cl, Br or I;
R3independently at each occurrence, is selected from alkyl, alkenyl, or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6OH, F, Cl, Br or I;
R4independently at each occurrence, is selected from alkyl, aryl, cycloalkyl or heterocyclyl; wherein each R 4Is optionally substituted with one, two, three or four groups independently selected from: r7F, Cl, Br or I; wherein each R4The aryl, cycloalkyl and heterocyclyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r8，C(O)R8，CO(O)R8F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，NR9C(O)OR9，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)OH，OH，CN，CF3，FCl, Br or I;
R6independently at each occurrence, is selected from alkyl or heterocyclyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: f, Cl, Br or I;
R7independently at each occurrence, is selected from aryl or heterocyclyl;
R8independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12OH，CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R 9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R12independently at each occurrence, is selected from alkyl, heterocyclyl or cycloalkyl; wherein each R12Optionally substituted with one or more alkoxy groups;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)NHR13，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13independently selected at each occurrenceFrom alkyl, alkenyl, alkynyl, aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r 14，OR14，SO2R14，NH2，NHR14，N(R14)2，NHC(O)R14，NHC(O)OR14，OH，CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SO2R15，C(O)R15，N(R15)2，NHC(O)R15，OH，CN，CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, OH, F, Cl, Br or I; wherein each R14The aryl, heterocyclyl and cycloalkyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted with one, two, three or four alkoxy groups; and
R16Independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In another embodiment of formula (Ic),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R2is alkyl, phenyl, cycloalkyl or heterocyclyl; wherein each R2Is optionally substituted with one, two, three or four groups independently selected from: r4，OR4，C(O)R4，CO(O)R4NHC(O)R4，NR4C(O)R4，C(O)NHR4Or C (O) N (R)4)2(ii) a Wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OR5，S O2R5，C(O)R5，CO(O)R5，NHR5，NHC(O)R5，NHS(O)2R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5，SO2NHR5Or CF3(ii) a Wherein each R2Optionally substituted with one F; wherein each R 2The heterocyclyl and cycloalkyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r5，OR5，C(O)R5，C(O)OR5，N(R5)2，NHC(O)R5Or C (O) NHR5；
R3Independently at each occurrence, is selected from alkyl, alkenyl, or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH;
R4independently at each occurrence, is selected from alkyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Optionally with one, two, three or four independently selected R7Substitution; wherein each R4The aryl, cycloalkyl and heterocyclyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r8，C(O)R8，CO(O)R8F, Cl or Br;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，C(O)R9，NH2，N(R9)2，NHC(O)R9，NR9C(O)OR9，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)OH，OH，CN，CF3Or F;
R6independently at each occurrence, is selected from alkyl or heterocyclyl;
R7independently at each occurrence, is selected from aryl or heterocyclyl;
R8independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R 8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12OH or CF3；
R9Independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R12independently at each occurrence, is selected from alkyl, heterocyclyl or cycloalkyl; wherein each R12Optionally substituted with one or more alkoxy groups;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)NHR13，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F or Cl;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R 13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SO2R14，NH2，NHR14，N(R14)2，NHC(O)R14，NHC(O)OR14OH or CF3(ii) a Wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidyl, pyrimidinyl, oxazolyl, pyrazolylThiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furyl, morpholinyl, isoxazolyl, cycloalkyl, and cycloalkenyl are optionally substituted with one, two, three, or four groups independently selected from: r15，OR15，SO2R15，C(O)R15，N(R15)2，NHC(O)R15，CN，OH，CF3F or Cl;
R14independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy or OH; wherein each R14The aryl, heterocyclyl and cycloalkyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH or Cl;
R15independently at each occurrence, is selected from alkyl; wherein R is 15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided thatWhen R is13When it is pyrrolinyl, X1、X2And X3Is N.
Yet another embodiment relates to compounds having formula (Ic), including
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (furo [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (thieno [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dihydro-1, 4-benzodioxin-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 3-fluoro-5- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-acetylphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 3-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (6-aminohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-benzodioxol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (pyridin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dihydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-propoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (2-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-2-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methyl-1H-indazol-5-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 5- ({4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } amino) -1H-indazole-3-carboxylate;
n- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (5-chloropyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1, 4-benzodioxin-6-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-fluorobenzoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methoxy-1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2R) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-propoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (dimethylamino) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-fluoro-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1, 3-benzodioxol-5-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-methoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- {4- [ (2-phenoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-hydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({1- [ (3S) -tetrahydrofuran-3-yl ] -1H-pyrazol-4-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 4-dioxa-8-azaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylthio) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (trifluoromethyl) thio ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-fluorophenyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (1H-imidazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (hydroxymethyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-benzodioxol-5-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-isopropyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (thiomorpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzylpiperidin-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-acetylamino-2-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [3- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-imidazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1- (3-cyanophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (2-hydroxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyanomethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclohexylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (dimethylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 4-dihydroisoquinolin-2 (1H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1H-indol-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (phenylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (diethylamino) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-phenylethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-aminophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
Tert-butyl (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } piperidin-4-yl) carbamate;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ 3-chloro-5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (cyclohexylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-chlorobenzyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (diethylcarbamoyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-hydroxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-6-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5, 6-dihydro [1, 2, 4] triazolo [4, 3-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-fluoropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylmethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3, 4, 9-tetrahydro-2H- β -carbolin-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tert-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [4- (trifluoromethyl) phenyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-difluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-benzylpyrrolidin-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-carbamoylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopropylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (methylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dioxolan-2-ylmethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (4-fluorophenyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-hydroxy-2-methylprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-phenyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (sec-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (ethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isobutyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4-carbamoylphenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (trifluoromethyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 6-dimethylmorpholin-4-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (prop-2-yn-1-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-cyanoethyl) (cyclopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (isopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -N-isopropyl- β -alanine;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5, 6-dimethoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-chlorophenoxy) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenyl-1, 3-thiazol-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid;
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (aminomethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (2-hydroxy-2-methylpropanoyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetylamino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (N, N-dimethylglycyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methoxyacetyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methylsulfonyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4, 4, 4-trifluorobutanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpentanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (benzyloxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ N- (2-furoyl) glycyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-thienyl) butyryl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-oxo-4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (N-benzoylglycyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenoxybutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (propionylamino) phenyl ] -amide;
n- [4- (pentanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (heptanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-4-enoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-methylpiperazin-1-yl) propionyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylate;
2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyclopentylethyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester;
n- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-methyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1E) -5-phenylpent-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1-benzyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxyethyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (1-propyl-1H-pyrazol-4-yl) pyridin-3-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-phenylpentyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [ 2-fluoro-4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 2-fluoro-4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (isopropylsulfonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-benzoylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (isopropylsulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (benzenesulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (benzoylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (butyrylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperazine-1-carboxylic acid tert-butyl ester;
n- [4- (4-propionylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopropylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-butanoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-isobutyryl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-benzoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [2- (3-methylbutyl) -2, 3-dihydro-1H-isoindol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexyloxy) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (4-chlorophenoxy) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (piperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n, N' -hexane-1, 6-diylbis (1, 3-dihydro-2H-isoindole-2-carboxylic acid amide);
n- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
ethyl 6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] hexanoate;
n-hexyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n-octyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (1-methyl-1H-pyrazol-4-yl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (methylamino) -6-oxohexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 6-oxo-6- [ (3-phenylpropyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (3-methylbutyl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (5- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-phenylpropyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-phenylpropyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4, 5, 6, 7, 8-hexahydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (8-fluoro-4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (morpholin-4-ylmethyl) -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-4, 5-dihydro-3H-2, 3-benzodiazepine-1-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (1-methylpiperidin-4-yl) oxy ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3R) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3S) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (azetidin-1-ylmethyl) -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperidine-1-carboxylic acid tert-butyl ester;
n- [4- (5-propyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (piperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [5- (3-methylbutyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (5-benzyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-chloropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-oxopyrrolidin-1-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxy-2, 3-dihydro-1H-inden-1-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-hydroxycyclopropyl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] -1H-benzimidazol-2-yl } piperazine-1-carboxylic acid tert-butyl ester;
n- [2- (piperazin-1-yl) -1H-benzoimidazol-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-benzoylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (tetrahydrofuran-3-yl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
N- (4- { [ (3-phenylpropyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- {4- [1- (4-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (tetrahydrofuran-3-ylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2S) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2R) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-phenylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-methoxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (2-hydroxyethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-3-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-4-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- (2-methoxyethyl) -N2- {4- [ (propylamino) carbonyl group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- (4-cyanophenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (trifluoromethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (tetrahydrofuran-3-ylmethyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-pyridin-2-ylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (1, 2-dihydroxyethyl) -N- {4- [ (propylamino) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (1 '-butyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and
n- [2- (4-acetylpiperazin-1-yl) -1H-benzimidazol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-D-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (ethoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (3-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-chlorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [3- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-furoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-thienylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (1H-pyrrol-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2, 5-dimethyl-1H-pyrrol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 3-thiazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3, 5-dimethyl-1, 2-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isonicotinoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridazin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrimidin-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- (4- {1- [3- (piperidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [6- (benzoylamino) hexyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (benzoylamino) methyl ] benzyl } carbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-L-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-D-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {4- [ (1-acetylpiperidin-4-yl) carbonyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-acetamidobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (methylsulfonyl) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-butyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isobutyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-methylbutyryl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 3, 3-trifluoropropionyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (methoxyacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopentylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclohexylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (2-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [3- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 4-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (3, 5-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (3, 4-dimethoxyphenyl) acetyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrrol-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrazol-5-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isonicotinyl piperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridazin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrazin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrimidin-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (N, N-dimethyl- β -alanyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-acetylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (phenylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1, 3-thiazol-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (morpholin-4-ylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxo-2, 3-dihydro-1H-isoindol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1- (2-phenylethyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- [2- (dimethylamino) ethyl group]-N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (morpholin-4-ylcarbonyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { benzyl [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutoxycarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 4- { [ (5-cyano-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoate;
n- (4- { (E) - [ (benzyloxy) imino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-aminopyrrolidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-methylbutyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-phenylpropyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- [4- ({ benzyl [3- (morpholin-4-yl) propyl ] amino } methyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-methyl-1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-methoxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (aminomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4- (methylthio) but-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3S) -1-hydroxy-3-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3R) -1, 3-dihydroxybutan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -1-hydroxyhex-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypentan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2R) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-cyclohexyl-3-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ (2R) -1-hydroxy-3- [ (4-methylbenzyl) thio ] propan-2-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-tert-butylphenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methoxy-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [6- (benzoylamino) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (2-methoxyethoxy) acetyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] pyrazin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6-acetamidohexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (1E) -3- [ benzyl (methyl) amino ] prop-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (4-phenoxypiperidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-phenoxyazetidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ benzyl (methyl) amino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-hydroxy-2-methylpropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbutyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [2- (2-oxopyrrolidin-1-yl) ethyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1-benzylpiperidin-4-yl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-phenylpropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (morpholin-4-yl) benzyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1-isobutyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxypropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {1 '- [ (2-methoxyethoxy) acetyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [4- (methylsulfonyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (ethoxyacetyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (cyclopentylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (2-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-cyanobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-cyanobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [3- (dimethylamino) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [4- (dimethylamino) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [3- (trifluoromethyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [4- (trifluoromethyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [3- (trifluoromethoxy) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 3-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 4-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 5-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (phenylacetyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (3-fluorophenyl) acetyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (morpholin-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [6- (benzoylamino) hexyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
4-fluoro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (pyridin-2-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (2-hydroxy-2-methylpropionyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {1 '- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (7-oxo-7- { [ (3R) -tetrahydrofuran-3-ylmethyl ] amino } heptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 7-oxo-7- [ (tetrahydro-2H-pyran-4-ylmethyl) amino ] heptyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (azetidin-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (morpholin-4-ylmethyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {5- [ (4-methylpiperazin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5- { [ (3-methylbutyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-hydroxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-chlorobenzoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [1 ' - (2-hydroxy-2-methylpropanoyl) -1 ', 2 ', 3 ', 6 ' -tetrahydro-2, 4 ' -bipyridin-5-yl ] -1, 3 ' -dihydro-2H-isoindole;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [1 ' - (2-hydroxy-2-methylpropanoyl) -1 ', 2 ', 3 ', 6 ' -tetrahydro-3, 4 ' -bipyridin-6-yl ] -1, 3 ' -dihydro-2H-isoindole;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-aminoethyl) -1H-imidazol-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2, 2-dimethyl-1, 3-dioxolan-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-methoxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4S) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4R) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } -2-oxoethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3- { benzyl [3- (morpholin-4-yl) propyl ] amino } -3-oxopropyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (6-bromo-2-oxoquinolin-1 (2H) -yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [6- (3-acetylphenyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (morpholin-4-ylacetyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (morpholin-4-ylacetyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (2- { (4-fluorobenzyl) [4- (pyridin-3-yl) benzyl ] amino } -1, 3-thiazol-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2-benzyl-1, 3-thiazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (7- { benzyl [3- (morpholin-4-yl) propyl ] amino } -7-oxoheptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-thiazol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (4-methylphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-dihydroxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (ethanesulfonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2, 3-dihydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1-hydroxy-4-methylpent-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (5- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.3] hept-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.4] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 9-diazaspiro [5.5] undecan-3-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { benzyl [3- (morpholin-4-yl) propyl ] amino } -4-oxobutyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4-phenylbutyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetyl-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butyrylamino) phenyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -pyrrolidin-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methoxybenzyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (2-oxa-7-azaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [6- (3-acetylphenyl) -4- (3-hydroxypropyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5- (acetamidomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [2- (2-chlorobenzyl) -1, 3-thiazol-4-yl ] -2-thienyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-fluorophenyl) butyl ] -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (3R) -1-isobutyrylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-benzoylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (methylsulfonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (2-hydroxypropan-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
{4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzyl } carbamic acid tert-butyl ester;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (methoxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (5- { [ (tetrahydrofuran-2-ylmethyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-methoxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (5- { [4- (2-methoxyethyl) piperazin-1-yl ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole;
n- [4- ({ [1- (morpholin-4-yl) cyclopentyl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-pentanoylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (1-acetylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (1-isobutyrylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl (2- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } ethyl) carbamate;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-phenylpropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (phenylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxyphenyl) acetyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-benzoylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-ethoxypropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (1-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpiperidin-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
Tert-butyl [ (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } azetidin-3-yl) methyl ] carbamate;
n- (4- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (morpholin-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (2, 3-dimethylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclohexylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tricyclo [ 3.3.1.1-3, 7- ] decan-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxycyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [4- (acetylamino) phenyl ] sulfonyl } amino) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (propylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-propylphenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (butanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ ({ [ (1S, 4R) -7, 7-dimethyl-2-oxobicyclo [2.2.1] hept-1-yl ] methyl } sulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (benzylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-fluorophenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (thiophen-2-ylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydro-2H-pyran-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (N, N-dimethylglycyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (4, 4-difluorocyclohexyl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (piperidin-1-ylsulfonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [1- (1, 3-thiazol-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -D-phenylpropanamide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -L-phenylpropanamide;
N- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (5-methyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-chloro-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-carbamoylbenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n2(Nalpha) - {4- [ (5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridin-6-ylcarbonyl) amino ] benzoyl } -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- [4- (4, 5, 6, 7-tetrahydro-1H-indazol-5-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-1-oxobutan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxyprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -1-cyanobutan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanocyclopropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (4-methyl-1, 3-thiazol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- [4- (butylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
1- {4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } azetidine-3-carboxylic acid methyl ester;
n- (4- {3- [ (3-methylbutyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (benzylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (cyclopentylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (cyclopentylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (2-methoxyethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopentylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrrolidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [ (dimethylamino) methyl ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 3-oxazol-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) (3-methylbutyryl) amino ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (9-chloro-5-oxo-2, 3, 3a, 4, 4a, 5-hexahydro-6H-furo [2 ', 3': 2, 3] cyclobuta [1, 2-c ] quinolin-6-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ 7-chloro-1- (2-hydroxyethyl) -3-oxo-1, 3-dihydrocyclobuta (cyclobuta) [ c ] quinolin-4 (2H) -yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (1-acetylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclopentylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (3, 5-dimethyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-difluoroethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -L-phenylalanine amide;
n- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiophen-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pyrimidin-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (5-oxo-L-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4, 4-difluorocyclohexyl) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (propan-2-yloxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-acetylpiperidin-4-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { 7-oxo-7- [ (3-phenylpropyl) amino ] heptyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (bicyclo [2.2.1] hept-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1, 3-thiazol-5-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-oxo-4, 5, 6, 7-tetrahydro-1-benzofuran-3-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {2- [ (3-methylbutyryl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (4-methylpentanoyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (ethoxyacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { [ (2-methoxyethoxy) acetyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-2-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [2- (benzoylamino) ethyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-3-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-L-prolyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-propionylazetidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pent-4-ynoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (thiophen-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethylglycyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethyl- β -alanyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrrolidin-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (pyrrolidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({1- [3- (piperidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methylpiperazin-1-yl) acetyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopropylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopentylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3-dimethylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (butanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (benzenesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-fluorophenyl) sulfonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propan-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (benzylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (thien-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -2-methylbutyryl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4, 4-difluorocyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-D-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (2-methylpentanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1, 2-oxazol-5-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridazin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrazin-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({1- [3- (piperidin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
trans-3- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] cyclobutanecarboxylic acid benzyl ester;
n- [4- (4- { [ (4-methylpiperazin-1-yl) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (benzoylamino) cyclohex-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (4- { [ (1-methylpiperidin-4-yl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydro-2H-thiopyran-4-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3R) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3S) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -2-methylbutyryl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (3-methylbutyryl) amino ] oxetan-3-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
4- ({4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } sulfonyl) piperidine-1-carboxylic acid tert-butyl ester;
n- {4- [4- (propylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methoxyethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (cyclopentylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (1, 4-dioxan-2-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopentylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (morpholin-4-ylcarbonyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopropylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [4- (but-2-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-dioxido-tetrahydro-2H-thiopyran-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { (4R) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (4S) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [ trans-3- (benzylcarbamoyl) cyclobutyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { trans-3- [ (2-phenylethyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { trans-3- [ (3-phenylpropyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methyl-1, 3-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (furan-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -3- (furan-2-yl) prop-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 3-oxazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (3, 3, 3-trifluoropropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 5-dimethyl-1H-pyrazol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methoxycyclohexyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 3-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-difluorocyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1H-pyrazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4[1- (tert-butoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-1, 2, 4-triazol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (3-ethoxypropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-hydroxy-3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-pyrrol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methylpropoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1-methyl prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-hydroxycyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1- { [1- (methoxymethyl) cyclopropyl ] carbonyl } -1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (methylsulfonyl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-acetyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -4-methylpent-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-methoxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopent-1-en-1-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (thiophen-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1-methyl-1H-pyrrol-2-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (4-methylhexanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-dimethylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-5-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclobutylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (piperidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [2- (pyrrolidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3S) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({ (3S) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (bicyclo [2.2.1] hept-2-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { cis-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopentylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and pharmaceutically acceptable salts thereof.
Yet another embodiment relates to compounds of formula (Ic) which are:
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
Yet another embodiment relates to compounds of formula (Ic) which are:
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
Embodiments of formula (IIc)
In another aspect, the present invention provides compounds of formula (IIc)
And pharmaceutically acceptable salts thereof; wherein X1、X2、X3As described herein for formula (Ic); r2Is phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein R is2Optionally according to R in formula (Ic) herein2The substituents above are substituted in the manner described.
In one embodiment of formula (IIc),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R2Is phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R2Optionally in the para-position byOne is independently selected from the following: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally independently selected by one, two, three or fourSubstituted with a group selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
Wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidyl, pyrimidine Optionally substituted with one, two, three or four groups independently selected from the group consisting of alkyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14Optionally substituted with one, two, three or four independently selected fromAnd (3) group substitution: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R 2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (IIc), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In addition to formula (IIc)In one embodiment, X1、X2And X3Is CH. In another embodiment of formula (IIc), X1And X3Is CH; x2Is N. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IIc), X2Is CH; x1And X3Is N. In another embodiment of formula (IIc), X2And X3Is CH; x1Is N. In another embodiment of formula (IIc), X1Is CH; x 2Is N; x3Is CR1. In another embodiment of formula (IIc), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IIc), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (IIc), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substitutedSubstituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), R1Is C (O) NH2. In another embodiment of formula (IIc), R1Is F. In another embodiment of formula (IIc), R1Is Cl. In another embodiment of formula (IIc), R1Is Br. In another embodiment of formula (IIc), R1Is CN. In another embodiment of formula (IIc), R1Is NH2. In another embodiment of formula (IIc), R 1Is NO2. In another embodiment of formula (IIc), R1Is CF3. In another embodiment of formula (IIc), R1Is C (O) OH. In another embodiment of formula (IIc), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by one or moreEach independently selected from the group consisting of: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X 1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (IIc), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl;wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X 2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X2And X3Is CH；X1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IIc), X 2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IIc), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIc)，X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is 6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a WhereinR3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIc), X 1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IIc), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Another embodiment relates to compounds having formula (IIc) including
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (furo [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (thieno [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dihydro-1, 4-benzodioxin-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 3-fluoro-5- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-acetylphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 3-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (6-aminohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (1, 3-benzodioxol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (3, 4-dihydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-propoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-2-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methyl-1H-indazol-5-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 5- ({4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } amino) -1H-indazole-3-carboxylate;
n- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (5-chloropyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1, 4-benzodioxin-6-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-fluorobenzoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (5-methoxy-1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-propoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (dimethylamino) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoro-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1, 3-benzodioxol-5-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- {4- [ (2-phenoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-hydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({1- [ (3S) -tetrahydrofuran-3-yl ] -1H-pyrazol-4-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 4-dioxa-8-azaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylthio) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (trifluoromethyl) thio ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (2-fluorophenyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (1H-imidazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (hydroxymethyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-benzodioxol-5-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-isopropyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ methyl (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiomorpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzylpiperidin-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-acetylamino-2-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({2- [3- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-imidazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1- (3-cyanophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (2-hydroxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyanomethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclohexylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 4-dihydroisoquinolin-2 (1H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1H-indol-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (phenylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (diethylamino) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-phenylethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-aminophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } piperidin-4-yl) carbamate;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ 3-chloro-5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (cyclohexylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-chlorobenzyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (diethylcarbamoyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-hydroxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-hydroxy-6-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5, 6-dihydro [1, 2, 4] triazolo [4, 3-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-fluoropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylmethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 3, 4, 9-tetrahydro-2H- β -carbolin-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tert-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [4- (trifluoromethyl) phenyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-difluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-benzylpyrrolidin-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-carbamoylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (cyclopropylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (methylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dioxolan-2-ylmethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (4-fluorophenyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-hydroxy-2-methylprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-phenyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-methoxyethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (sec-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (ethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isobutyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4-carbamoylphenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (trifluoromethyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 6-dimethylmorpholin-4-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (prop-2-yn-1-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ isopropyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyanoethyl) (cyclopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (isopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -N-isopropyl- β -alanine;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5, 6-dimethoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-chlorophenoxy) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenyl-1, 3-thiazol-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid;
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (aminomethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (2-hydroxy-2-methylpropanoyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetylamino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (N, N-dimethylglycyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methoxyacetyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methylsulfonyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4, 4, 4-trifluorobutanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-methylpentanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (benzyloxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ N- (2-furoyl) glycyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-thienyl) butyryl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-oxo-4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (N-benzoylglycyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenoxybutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (propionylamino) phenyl ] -amide;
n- [4- (pentanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (heptanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (pent-4-enoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-methylpiperazin-1-yl) propionyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylate;
2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyclopentylethyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester;
n- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-methyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1E) -5-phenylpent-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxyethyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (1-propyl-1H-pyrazol-4-yl) pyridin-3-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-phenylpentyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [ 2-fluoro-4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 2-fluoro-4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (isopropylsulfonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-benzoylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (isopropylsulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (benzenesulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (benzoylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (butyrylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperazine-1-carboxylic acid tert-butyl ester;
N- [4- (4-propionylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopropylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-butanoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-isobutyryl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-benzoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [2- (3-methylbutyl) -2, 3-dihydro-1H-isoindol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexyloxy) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (5- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-phenylpropyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-phenylpropyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4, 5, 6, 7, 8-hexahydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (8-fluoro-4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (morpholin-4-ylmethyl) -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-4, 5-dihydro-3H-2, 3-benzodiazepine-1-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (1-methylpiperidin-4-yl) oxy ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3R) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3S) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (azetidin-1-ylmethyl) -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperidine-1-carboxylic acid tert-butyl ester;
n- [4- (5-propyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (piperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [5- (3-methylbutyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-benzyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-chloropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-oxopyrrolidin-1-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxy-2, 3-dihydro-1H-inden-1-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-hydroxycyclopropyl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] -1H-benzimidazol-2-yl } piperazine-1-carboxylic acid tert-butyl ester;
n- [2- (piperazin-1-yl) -1H-benzoimidazol-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-benzoylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (tetrahydrofuran-3-yl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- (4- { [ (3-phenylpropyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- {4- [1- (4-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (tetrahydrofuran-3-ylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2S) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2R) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-phenylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-methoxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (2-hydroxyethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-3-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-4-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- (2-methoxyethyl) -N2- {4- [ (propylamino) carbonyl group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- (4-cyanophenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (trifluoromethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (tetrahydrofuran-3-ylmethyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-pyridin-2-ylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (1, 2-dihydroxyethyl) -N- {4- [ (propylamino) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-butyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and
n- [2- (4-acetylpiperazin-1-yl) -1H-benzimidazol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-D-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (ethoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-chlorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [3- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [4- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-furoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-thienylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrrol-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2, 5-dimethyl-1H-pyrrol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 3-thiazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3, 5-dimethyl-1, 2-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (pyridin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isonicotinoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridazin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrimidin-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- (4- {1- [3- (piperidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [6- (benzoylamino) hexyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({4- [ (benzoylamino) methyl ] benzyl } carbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-L-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-D-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (1-acetylpiperidin-4-yl) carbonyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-acetamidobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (methylsulfonyl) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-butyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isobutyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-methylbutyryl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 3, 3-trifluoropropionyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (methoxyacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopentylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclohexylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {4- [3- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 4-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 5-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (3, 4-dimethoxyphenyl) acetyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrrol-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrazol-5-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (4-isonicotinyl piperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridazin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrazin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrimidin-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (N, N-dimethyl- β -alanyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-acetylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (phenylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1, 3-thiazol-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (morpholin-4-ylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxo-2, 3-dihydro-1H-isoindol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1- (2-phenylethyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- [2- (dimethylamino) ethyl group]-N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (morpholin-4-ylcarbonyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { benzyl [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutoxycarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
Methyl 4- { [ (5-cyano-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoate;
n- (4- { (E) - [ (benzyloxy) imino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-oxindole-2-carboxamide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-aminopyrrolidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-methylbutyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-phenylpropyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- [4- ({ benzyl [3- (morpholin-4-yl) propyl ] amino } methyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-methyl-1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-methoxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (aminomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4- (methylthio) but-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S, 3S) -1-hydroxy-3-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3R) -1, 3-dihydroxybutan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxyhex-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypentan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2R) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-cyclohexyl-3-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ (2R) -1-hydroxy-3- [ (4-methylbenzyl) thio ] propan-2-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-tert-butylphenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methoxy-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (2-methoxyethoxy) acetyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] pyrazin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { (1E) -3- [ benzyl (methyl) amino ] prop-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-phenoxypiperidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-phenoxyazetidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ benzyl (methyl) amino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-hydroxy-2-methylpropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbutyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [2- (2-oxopyrrolidin-1-yl) ethyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1-benzylpiperidin-4-yl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-phenylpropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [4- (morpholin-4-yl) benzyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxypropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {1 '- [ (2-methoxyethoxy) acetyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (morpholin-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c1 pyridine-2-carboxamide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c1 pyridine-2-carboxamide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (2-hydroxy-2-methylpropionyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (azetidin-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (morpholin-4-ylmethyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-methylpiperazin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5- { [ (3-methylbutyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-hydroxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [1 ' - (2-hydroxy-2-methylpropanoyl) -1 ', 2 ', 3 ', 6 ' -tetrahydro-2, 4 ' -bipyridin-5-yl ] -1, 3 ' -dihydro-2H-isoindole;
N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-oxindole-2-carboxamide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {1 '- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [1 ' - (2-hydroxy-2-methylpropanoyl) -1 ', 2 ', 3 ', 6 ' -tetrahydro-3, 4 ' -bipyridin-6-yl ] -1, 3 ' -dihydro-2H-isoindole;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-aminoethyl) -1H-imidazol-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2, 2-dimethyl-1, 3-dioxolan-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-methoxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4S) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4R) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } -2-oxoethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3- { benzyl [3- (morpholin-4-yl) propyl ] amino } -3-oxopropyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (morpholin-4-ylacetyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (morpholin-4-ylacetyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (2- { (4-fluorobenzyl) [4- (pyridin-3-yl) benzyl ] amino } -1, 3-thiazol-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2-benzyl-1, 3-thiazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-thiazol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (4-methylphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-dihydroxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (ethanesulfonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2, 3-dihydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1-hydroxy-4-methylpent-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (5- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.3] hept-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.4] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 9-diazaspiro [5.5] undecan-3-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { benzyl [3- (morpholin-4-yl) propyl ] amino } -4-oxobutyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetyl-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butyrylamino) phenyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -pyrrolidin-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methoxybenzyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl- } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (2-oxa-7-azaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5- (acetamidomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [2- (2-chlorobenzyl) -1, 3-thiazol-4-yl ] -2-thienyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (3R) -1-isobutyrylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-benzoylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({ [1- (methylsulfonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (2-hydroxypropan-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
{4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzyl } carbamic acid tert-butyl ester;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (methoxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5- { [ (tetrahydrofuran-2-ylmethyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-methoxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (5- { [4- (2-methoxyethyl) piperazin-1-yl ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole;
n- [4- ({ [1- (morpholin-4-yl) cyclopentyl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-pentanoylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (1-acetylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (1-isobutyrylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl (2- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } ethyl) carbamate;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-phenylpropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (phenylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrido [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxyphenyl) acetyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-benzoylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-ethoxypropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (1-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpiperidin-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
Tert-butyl [ (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } azetidin-3-yl) methyl ] carbamate;
n- (4- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (morpholin-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (2, 3-dimethylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclohexylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tricyclo [ 3.3.1.1-3, 7- ] decan-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxycyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [4- (acetylamino) phenyl ] sulfonyl } amino) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (propylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-propylphenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (butanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ ({ [ (1S, 4R) -7, 7-dimethyl-2-oxobicyclo [2.2.1] hept-1-yl ] methyl } sulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (benzylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-fluorophenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (thiophen-2-ylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydro-2H-pyran-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (N, N-dimethylglycyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (4, 4-difluorocyclohexyl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (piperidin-1-ylsulfonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [1- (1, 3-thiazol-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Na1pha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -D-phenylpropanamide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Na1pha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -L-phenylpropanamide;
N- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (5-methyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-chloro-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-carbamoylbenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n2(Na1pha) - {4- [ (5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridin-6-ylcarbonyl) amino ] benzoyl } -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- [4- (4, 5, 6, 7-tetrahydro-1H-indazol-5-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-1-oxobutan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxyprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -1-cyanobutan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrido [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanocyclopropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (4-methyl-1, 3-thiazol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- [4- (butylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
1- {4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } azetidine-3-carboxylic acid methyl ester;
n- (4- {3- [ (3-methylbutyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (benzylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (cyclopentylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (cyclopentylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (2-methoxyethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopentylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrrolidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [ (dimethylamino) methyl ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 3-oxazol-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (2-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (3, 5-dimethyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-difluoroethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -L-phenylalanine amide;
n- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiophen-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pyrimidin-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (5-oxo-L-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-acetylpiperidin-4-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (cyclopentylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (bicyclo [2.2.1] hept-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1, 3-thiazol-5-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-oxo-4, 5, 6, 7-tetrahydro-1-benzofuran-3-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {2- [ (3-methylbutyryl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (4-methylpentanoyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (ethoxyacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { [ (2-methoxyethoxy) acetyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-2-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [2- (benzoylamino) ethyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-3-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-L-prolyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-propionylazetidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (pent-4-ynoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (thiophen-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethylglycyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethyl- β -alanyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (pyrrolidin-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (pyrrolidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (piperidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methylpiperazin-1-yl) acetyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopropylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopentylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3, 3-dimethylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (butanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (benzenesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-fluorophenyl) sulfonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (ethanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propan-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (benzylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (thien-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -2-methylbutyryl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4, 4-difluorocyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (5-oxo-D-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpentanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1, 2-oxazol-5-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridazin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrazin-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (pyrimidin-4-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (piperidin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
trans-3- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] cyclobutanecarboxylic acid benzyl ester;
n- [4- (4- { [ (4-methylpiperazin-1-yl) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (benzoylamino) cyclohex-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1-methylpiperidin-4-yl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydro-2H-thiopyran-4-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3R) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3S) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -2-methylbutyryl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (3-methylbutyryl) amino ] oxetan-3-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
4- ({4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } sulfonyl) piperidine-1-carboxylic acid tert-butyl ester;
n- {4- [4- (propylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methoxyethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (cyclopentylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (1, 4-dioxan-2-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopentylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (morpholin-4-ylcarbonyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [4- (cyclopropylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (but-2-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-dioxido-tetrahydro-2H-thiopyran-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { (4R) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (4S) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [ trans-3- (benzylcarbamoyl) cyclobutyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { trans-3- [ (2-phenylethyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { trans-3- [ (3-phenylpropyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methyl-1, 3-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (furan-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -3- (furan-2-yl) prop-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (1, 3-oxazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3, 3, 3-trifluoropropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 5-dimethyl-1H-pyrazol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methoxycyclohexyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 3-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-difluorocyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1H-pyrazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tert-butoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [3- (1H-1, 2, 4-triazol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-ethoxypropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-hydroxy-3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-pyrrol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methylpropoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1-methyl prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1-hydroxycyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1- { [1- (methoxymethyl) cyclopropyl ] carbonyl } -1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (methylsulfonyl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-acetyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -4-methylpent-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-methoxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopent-1-en-1-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (thiophen-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2, 2-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrrol-2-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (4-methylhexanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-dimethylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-5-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclobutylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (piperidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [2- (pyrrolidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (trans-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({ (3S) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3S) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (bicyclo [2.2.1] hept-2-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { cis-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopentylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and pharmaceutically acceptable salts thereof.
Embodiments of formula (IIIc)
In another aspect, the invention provides a compound of formula (IIIc)
And pharmaceutically acceptable salts thereof; wherein X1、X2、X3As described herein for formula (Ic); when R is2When it is phenyl, RXAs described herein for the substituent in the para position of formula (Ic).
In one embodiment of formula (IIIc),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
RxIs R5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I;
R3independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R 3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is 3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinylPyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothien-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazole The aryl, cycloalkyl, and cycloalkenyl groups are optionally substituted with one, two, three, or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl, wherein R is15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when X is1、X2And X3When is CH, RxIs not methyl;
provided that when X is1、X2And X3When is CH, RxIs not methoxy;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X 1、X2And X3Is N.
In one embodiment of formula (IIIc), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is C H; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (IIIc), X1、X2And X3Is CH. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is N. In thatIn another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IIIc), X2Is CH; x1And X3Is N. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is N. In another embodiment of formula (IIIc), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (IIIc), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IIIc), X1Is N; x2Is CR 1；X3Is CH. In another embodiment of formula (IIIc), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IIIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), R 1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH;wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), R1Is C (O) NH2. In another embodiment of formula (IIIc), R1Is F. In another embodiment of formula (IIIc), R1Is Cl. In another embodiment of formula (IIIc), R1Is Br. In another embodiment of formula (IIIc), R1Is CN. In another embodiment of formula (IIIc), R1Is NH2. In another embodiment of formula (IIIc), R1Is NO2. In another embodiment of formula (IIIc), R 1Is CF3. In another embodiment of formula (IIIc), R1Is C (O) OH. In another embodiment of formula (IIIc), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH;wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from:R6，OR6，NH2，NHC(O)R6，N(R6)2or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X 1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; it is composed ofWherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is 3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IIIc), X2And X3Is CH; x 1Is CR1；R1Is NO2. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1Is CH; x2And X 3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected fromGroup substitution: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (IIIc)，X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In one embodiment of formula (IIIc), RxIs R5，OR5，SO2R5，C(O)R5，CO(O)R3，NHR5，NHC(O)R5，NHS(O)2R5，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOR5，SO2NHR5Or CF3. In another embodiment of formula (IIIc), R xIs R5，R5Is a heterocyclyl group, which is optionally substituted as described in the embodiments herein.
In another embodiment of formula (IIIc), RxIs phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, pyrrolo [1, 2-d][1，2，4]Triazin-1 (2H) -one, isoindolin-1-one or 1, 2, 3, 6-tetrahydropyridinyl. In another embodiment of formula (IIIc), RxIs phthalazin-1 (2H) -keto, isoquinolinyl, isoquinolin-1 (2H) -keto, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -keto, 5-fluorophthalazin-1 (2H) -keto,(Z) -3H-benzo [ d ]][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, isoindolin-1-keto, or pyrrolo [1, 2-d ]][1，2，4]Triazin-1 (2H) -one; which is optionally substituted as defined herein. In another embodiment of formula (IIIc), RxIs, 2, 3, 6-tetrahydropyridinyl; which is optionally substituted as defined herein.
Yet another embodiment relates to compounds having formula (IIIc) including
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (furo [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (thieno [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 3-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dihydro-1, 4-benzodioxin-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 3-fluoro-5- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-acetylphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 3-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (6-aminohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-benzodioxol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dihydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-propoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-2-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methyl-1H-indazol-5-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 5- ({4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } amino) -1H-indazole-3-carboxylate;
n- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (5-chloropyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1, 4-benzodioxin-6-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (2-fluorobenzoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methoxy-1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-propoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({2- [4- (dimethylamino) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoro-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1, 3-benzodioxol-5-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- {4- [ (2-phenoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-hydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (3-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({1- [ (3S) -tetrahydrofuran-3-yl ] -1H-pyrazol-4-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 4-dioxa-8-azaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylthio) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (trifluoromethyl) thio ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-fluorophenyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (1H-imidazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (hydroxymethyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-benzodioxol-5-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-isopropyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiomorpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzylpiperidin-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-acetylamino-2-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (3, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [3- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-imidazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1- (3-cyanophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (2-hydroxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyanomethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclohexylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 4-dihydroisoquinolin-2 (1H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1H-indol-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (phenylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (diethylamino) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-hydroxy-2-phenylethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-aminophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } piperidin-4-yl) carbamate;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ 3-chloro-5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (cyclohexylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-chlorobenzyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (diethylcarbamoyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (2-hydroxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-6-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5, 6-dihydro [1, 2, 4] triazolo [4, 3-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-fluoropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylmethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3, 4, 9-tetrahydro-2H- β -carbolin-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tert-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [4- (trifluoromethyl) phenyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-difluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-benzylpyrrolidin-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-carbamoylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopropylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (methylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dioxolan-2-ylmethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (4-fluorophenyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-hydroxy-2-methylprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-phenyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({2- [4- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (sec-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (ethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isobutyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4-carbamoylphenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (trifluoromethyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 6-dimethylmorpholin-4-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (prop-2-yn-1-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyanoethyl) (cyclopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (isopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -N-isopropyl- β -alanine;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5, 6-dimethoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-chlorophenoxy) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenyl-1, 3-thiazol-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid;
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (aminomethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (2-hydroxy-2-methylpropanoyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetylamino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (N, N-dimethylglycyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methoxyacetyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methylsulfonyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4, 4, 4-trifluorobutanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-methylpentanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (benzyloxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ N- (2-furoyl) glycyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-thienyl) butyryl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-oxo-4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (N-benzoylglycyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenoxybutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (propionylamino) phenyl ] -amide;
n- [4- (pentanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (heptanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (pent-4-enoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-methylpiperazin-1-yl) propionyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylate;
2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyclopentylethyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester;
n- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-methyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1E) -5-phenylpent-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxyethyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-phenylpentyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (isopropylsulfonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-benzoylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (isopropylsulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (benzenesulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (benzoylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (butyrylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperazine-1-carboxylic acid tert-butyl ester;
n- [4- (4-propionylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopropylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexyloxy) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4, 5, 6, 7, 8-hexahydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (8-fluoro-4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (morpholin-4-ylmethyl) -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-4, 5-dihydro-3H-2, 3-benzodiazepine-1-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (1-methylpiperidin-4-yl) oxy ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3R) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3S) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (azetidin-1-ylmethyl) -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperidine-1-carboxylic acid tert-butyl ester;
n- [4- (5-propyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (piperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [5- (3-methylbutyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (5-benzyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-chloropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-oxopyrrolidin-1-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxy-2, 3-dihydro-1H-inden-1-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-hydroxycyclopropyl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-benzoylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (tetrahydrofuran-3-yl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- (4- { [ (3-phenylpropyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- {4- [1- (4-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1-benzyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (tetrahydrofuran-3-ylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2S) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2R) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-phenylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-methoxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (2-hydroxyethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-3-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-4-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- (2-methoxyethyl) -N2- {4- [ (propylamino) carbonyl group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- (4-cyanophenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (trifluoromethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (tetrahydrofuran-3-ylmethyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-pyridin-2-ylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (1, 2-dihydroxyethyl) -N- {4- [ (propylamino) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-D-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (ethoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (3-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-chlorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [3- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [4- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-furoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-thienylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrrol-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2, 5-dimethyl-1H-pyrrol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 3-thiazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3, 5-dimethyl-1, 2-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (pyridin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isonicotinoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridazin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrimidin-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- (4- {1- [3- (piperidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [6- (benzoylamino) hexyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (benzoylamino) methyl ] benzyl } carbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (5-oxo-L-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-D-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (1-acetylpiperidin-4-yl) carbonyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-acetamidobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (methylsulfonyl) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-butyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isobutyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-methylbutyryl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 3, 3-trifluoropropionyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (methoxyacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (cyclopentylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclohexylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [3- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (3, 4-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 5-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (3, 4-dimethoxyphenyl) acetyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrrol-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrazol-5-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isonicotinyl piperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridazin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrazin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (pyrimidin-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (N, N-dimethyl- β -alanyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-acetylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (phenylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1, 3-thiazol-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (morpholin-4-ylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1w isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxo-2, 3-dihydro-1H-isoindol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N5- [2- (dimethylamino) ethyl group]-N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (morpholin-4-ylcarbonyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { benzyl [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutoxycarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 4- { [ (5-cyano-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoate;
n- (4- { (E) - [ (benzyloxy) imino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-aminopyrrolidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- [4- ({ benzyl [3- (morpholin-4-yl) propyl ] amino } methyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-methyl-1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-methoxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (aminomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4- (methylthio) but-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S, 3S) -1-hydroxy-3-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3R) -1, 3-dihydroxybutan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxyhex-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypentan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2R) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-cyclohexyl-3-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ (2R) -1-hydroxy-3- [ (4-methylbenzyl) thio ] propan-2-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-tert-butylphenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methoxy-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (1E) -3- [ benzyl (methyl) amino ] prop-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-phenoxypiperidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-phenoxyazetidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ benzyl (methyl) amino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-hydroxy-2-methylpropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbutyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (tetrahydrofuran-3-ylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [2- (2-oxopyrrolidin-1-yl) ethyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1-benzylpiperidin-4-yl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-phenylpropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (morpholin-4-yl) benzyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxypropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (morpholin-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (azetidin-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (morpholin-4-ylmethyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {5- [ (4-methylpiperazin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5- { [ (3-methylbutyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-hydroxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-aminoethyl) -1H-imidazol-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2, 2-dimethyl-1, 3-dioxolan-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-methoxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4S) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4R) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } -2-oxoethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3- { benzyl [3- (morpholin-4-yl) propyl ] amino } -3-oxopropyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2-benzyl-1, 3-thiazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-thiazol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (4-methylphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-dihydroxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (ethanesulfonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2, 3-dihydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1-hydroxy-4-methylpent-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.3] hept-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.4] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 9-diazaspiro [5.5] undecan-3-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { benzyl [3- (morpholin-4-yl) propyl ] amino } -4-oxobutyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetyl-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butyrylamino) phenyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -pyrrolidin-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methoxybenzyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (2-oxa-7-azaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5- (acetamidomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (3R) -1-isobutyrylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-benzoylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (methylsulfonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (2-hydroxypropan-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
{4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzyl } carbamic acid tert-butyl ester;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (methoxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (5- { [ (tetrahydrofuran-2-ylmethyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-methoxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (5- { [4- (2-methoxyethyl) piperazin-1-yl ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole;
n- [4- ({ [1- (morpholin-4-yl) cyclopentyl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-pentanoylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
tert-butyl (2- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } ethyl) carbamate;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (3, 3, 3-trifluoropropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-phenylpropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (phenylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxyphenyl) acetyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (methoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-benzoylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-ethoxypropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (1-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (1-methylpiperidin-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl [ (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } azetidin-3-yl) methyl ] carbamate;
n- (4- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (morpholin-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (2, 3-dimethylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (2, 2-dimethylpropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tricyclo [ 3.3.1.1-3, 7- ] decan-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxycyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [4- (acetylamino) phenyl ] sulfonyl } amino) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (propylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-propylphenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (butanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ ({ [ (1S, 4R) -7, 7-dimethyl-2-oxobicyclo [2.2.1] hept-1-yl ] methyl } sulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (ethanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (benzylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-fluorophenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (thiophen-2-ylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (N, N-dimethylglycyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (4, 4-difluorocyclohexyl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (piperidin-1-ylsulfonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [1- (1, 3-thiazol-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -D-phenylpropanamide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (5-methyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-chloro-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (2-carbamoylbenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n2(Nalpha) - {4- [ (5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridin-6-ylcarbonyl) amino ] benzoyl } -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (4, 5, 6, 7-tetrahydro-1H-indazol-5-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-1-oxobutan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxyprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -1-cyanobutan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanocyclopropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (4-methyl-1, 3-thiazol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
1- {4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } azetidine-3-carboxylic acid methyl ester;
N- (4- {3- [ (3-methylbutyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (benzylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (cyclopentylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (cyclopentylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (2-methoxyethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopentylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrrolidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [ (dimethylamino) methyl ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-oxazol-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (3, 5-dimethyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-difluoroethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -L-phenylalanine amide;
N- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiophen-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (pyrimidin-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (5-oxo-L-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-acetylpiperidin-4-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (bicyclo [2.2.1] hept-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1, 3-thiazol-5-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-oxo-4, 5, 6, 7-tetrahydro-1-benzofuran-3-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {2- [ (3-methylbutyryl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (4-methylpentanoyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (ethoxyacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { [ (2-methoxyethoxy) acetyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-2-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [2- (benzoylamino) ethyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-3-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-L-prolyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-propionylazetidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pent-4-ynoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (thiophen-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethylglycyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethyl- β -alanyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrrolidin-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (pyrrolidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({1- [3- (piperidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methylpiperazin-1-yl) acetyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopropylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopentylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3-dimethylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (butanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (benzenesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-fluorophenyl) sulfonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propan-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (benzylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (thien-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -2-methylbutyryl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4, 4-difluorocyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-D-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (2-methylpentanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1, 2-oxazol-5-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridazin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrazin-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({1- [3- (piperidin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (4-methylpiperazin-1-yl) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (benzoylamino) cyclohex-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1-methylpiperidin-4-yl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (4- { [ (1, 1-tetrahydro-2H-thiopyran-4-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3R) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3S) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -2-methylbutyryl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (3-methylbutyryl) amino ] oxetan-3-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
4- ({4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } sulfonyl) piperidine-1-carboxylic acid tert-butyl ester;
n- {4- [4- (propylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methoxyethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (cyclopentylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (1, 4-dioxan-2-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopentylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (morpholin-4-ylcarbonyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopropylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (but-2-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-dioxido-tetrahydro-2H-thiopyran-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { (4R) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (4S) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methyl-1, 3-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (furan-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -3- (furan-2-yl) prop-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 3-oxazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3, 3, 3-trifluoropropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 5-dimethyl-1H-pyrazol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methoxycyclohexyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 3-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-difluorocyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (1H-pyrazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tert-butoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-1, 2, 4-triazol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-ethoxypropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-hydroxy-3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-pyrrol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methylpropoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (1-methyl prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-hydroxycyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1- { [1- (methoxymethyl) cyclopropyl ] carbonyl } -1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (methylsulfonyl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-acetyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -4-methylpent-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-methoxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopent-1-en-1-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (thiophen-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclohexylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrrol-2-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (4-methylhexanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-dimethylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-5-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclobutylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (piperidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [2- (pyrrolidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (trans-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (3S) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3S) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3S) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { cis-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopentylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and pharmaceutically acceptable salts thereof.
Yet another embodiment relates to compounds having formula (IIIc) including
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4, 5, 6, 7, 8-hexahydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (8-fluoro-4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (morpholin-4-ylmethyl) -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-4, 5-dihydro-3H-2, 3-benzodiazepine-1-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (1-methylpiperidin-4-yl) oxy ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3R) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3S) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (azetidin-1-ylmethyl) -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-2, 3-dihydro-1H-isoindol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and pharmaceutically acceptable salts thereof.
Embodiments of formula (IVc)
In another aspect, the present invention provides a compound of formula (IVc)
And pharmaceutically acceptable salts thereof; wherein X1、X2、X3And R5As described herein for formula (Ic).
In one embodiment of formula (IVc),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R 3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is 3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (IVc), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x 1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (IVc), X1、X2And X3Is CH. In another embodiment of formula (IVc), X1And X3Is CH; x2Is N. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1. In another embodiment of formula (IVc), X2Is CH; x1And X3Is N. In another embodiment of formula (IVc), X2And X3Is CH; x1Is N. In another embodiment of formula (IVc), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (IVc), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (IVc), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (IVc), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (IVc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl groupOptionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), R1Is C (O) NH2. In another embodiment of formula (IVc), R1Is F. In another embodiment of formula (IVc), R1Is Cl. In another embodiment of formula (IVc), R1Is Br. In another embodiment of formula (IVc), R1Is CN. In another embodiment of formula (IVc), R1Is NH2. In another embodiment of formula (IVc), R1Is NO2. In another embodiment of formula (IVc), R1Is CF3. In another embodiment of formula (IVc), R1Is C (O) OH. In another embodiment of formula (IVc), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVc), X 1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally independently selected by one or moreSubstituted with a group selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1And X3Is C H; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is Br. In addition to formula (IVc)In one embodiment, X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR 1；R1Is NO2. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (IVc), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is OR 3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; it is composed ofWherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (IVc), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (IVc), X 1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected fromAnd (3) substitution: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is NO 2. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (IVc), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds having formula (IVc), including
N- {4- [ (4, 4, 4-trifluorobutanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpentanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (benzyloxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ N- (2-furoyl) glycyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-thienyl) butyryl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-oxo-4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (N-benzoylglycyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenoxybutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (propionylamino) phenyl ] -amide;
n- [4- (pentanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (heptanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-4-enoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-methylpiperazin-1-yl) propionyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylate;
2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-methyl-1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (Ring)Pentylacetyl) amino]Phenyl } -N5- (2-methoxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (aminomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methoxy-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (morpholin-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetyl-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butyrylamino) phenyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5- (acetamidomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (2-hydroxypropan-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (methoxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-acetylpiperidin-4-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (bicyclo [2.2.1] hept-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1, 3-thiazol-5-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (4-oxo-4, 5, 6, 7-tetrahydro-1-benzofuran-3-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
Embodiments of formula (Vc)
In another aspect, the present invention provides a compound of formula (Vc)
And pharmaceutically acceptable salts thereof; wherein X1、X2、X3And R5As described herein for formula (Ic).
In one embodiment of formula (Vc),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r 9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, arylA group, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl group, furanAnd [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R 13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothien-3-yl 1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or more substituentsFour groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r 16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence is selected fromAlkyl radical, wherein R15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (Vc), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (Vc), X1、X2And X3Is CH. In another embodiment of formula (Vc), X1And X3Is CH; x2Is N. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1. In another embodiment of formula (Vc), X 1Is CH; x2And X3Is CR1. In another embodiment of formula (Vc), X2Is CH;X1and X3Is N. In another embodiment of formula (Vc), X2And X3Is CH; x1Is N. In another embodiment of formula (Vc), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (Vc), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (Vc), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (Vc), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (Vc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Vc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl groupOptionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), R1Is C (O) NH2. In another embodiment of formula (Vc), R1Is F. In another embodiment of formula (Vc), R 1Is Cl. In another embodiment of formula (Vc), R1Is Br. In another embodiment of formula (Vc), R1Is CN. In another embodiment of formula (Vc), R1Is NH2. In another embodiment of formula (Vc), R1Is NO2. In another embodiment of formula (Vc), R1Is CF3. In another embodiment of formula (Vc), R1Is C (O) OH. In another embodiment of formula (Vc), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X 1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (Vc), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (Vc), X2And X3Is CH; x 1Is CR1；R1Is Br. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is CN. In another of formula (Vc)In one embodiment, X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (Vc), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another of formula (Vc)In one embodiment, X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X 1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (Vc), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds having formula (Vc), including
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 3-dihydro-1, 4-benzodioxin-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 3-fluoro-5- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 3-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (6-aminohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-benzodioxol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dihydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-propoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-2-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methyl-1H-indazol-5-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 5- ({4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } amino) -1H-indazole-3-carboxylate;
n- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1, 4-benzodioxin-6-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methoxy-1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (2-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-propoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (dimethylamino) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoro-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 3-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1, 3-benzodioxol-5-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (4-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- {4- [ (2-phenoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-hydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({1- [ (3S) -tetrahydrofuran-3-yl ] -1H-pyrazol-4-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (methylthio) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (trifluoromethyl) thio ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (1H-imidazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (hydroxymethyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 3-benzodioxol-5-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-isopropyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzylpiperidin-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-acetylamino-2-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- ({2- [3- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-imidazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1- (3-cyanophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyanomethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (cyclohexylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (phenylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (diethylamino) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-aminophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-chlorobenzyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-hydroxy-6-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-fluoropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tert-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-benzylpyrrolidin-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (cyclopropylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (methylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (4-fluorophenyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-hydroxy-2-methylprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-phenyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (sec-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (prop-2-yn-1-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5, 6-dimethoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-chlorophenoxy) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenyl-1, 3-thiazol-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid;
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (aminomethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (2-hydroxy-2-methylpropanoyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetylamino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (N, N-dimethylglycyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methoxyacetyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methylsulfonyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-chloropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-hydroxy-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-oxopyrrolidin-1-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxy-2, 3-dihydro-1H-inden-1-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-hydroxycyclopropyl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- (4- { [ (3-phenylpropyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
5-fluoro-N- [4- ({ [ (2S) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2R) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-phenylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-3-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-4-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- (2-methoxyethyl) -N2- {4- [ (propylamino) carbonyl group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (tetrahydrofuran-3-ylmethyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (1, 2-dihydroxyethyl) -N- {4- [ (propylamino) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [6- (benzoylamino) hexyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (benzoylamino) methyl ] benzyl } carbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N5- [2- (dimethylamino) ethyl group]-N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (morpholin-4-ylcarbonyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutoxycarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4- (methylthio) but-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S, 3S) -1-hydroxy-3-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3R) -1, 3-dihydroxybutan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxyhex-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypentan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2R) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-cyclohexyl-3-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ (2R) -1-hydroxy-3- [ (4-methylbenzyl) thio ] propan-2-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-tert-butylphenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5- (hydroxymethyl) -N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-hydroxy-2-methylpropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2, 2-dimethyl-1, 3-dioxolan-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-methoxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4S) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4R) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-thiazol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (4-methylphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-dihydroxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2, 3-dihydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1-hydroxy-4-methylpent-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -pyrrolidin-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (3R) -1-isobutyrylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-benzoylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({ [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (methylsulfonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (morpholin-4-yl) cyclopentyl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [1- (1, 3-thiazol-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -D-phenylpropanamide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -L-phenylpropanamide;
N- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (5-methyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-chloro-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-carbamoylbenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n2(Nalpha) - {4- [ (5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridin-6-ylcarbonyl) amino ] benzoyl } -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (4, 5, 6, 7-tetrahydro-1H-indazol-5-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-1-oxobutan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxyprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (cyclopentylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -1-cyanobutan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanocyclopropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (4-methyl-1, 3-thiazol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- [4- (butylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [ (dimethylamino) methyl ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-oxazol-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (3, 5-dimethyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 2-difluoroethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -L-phenylalanine amide;
n- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (thiophen-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pyrimidin-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and pharmaceutically acceptable salts thereof.
Embodiments of formula (VIc)
In another aspect, the present invention provides a compound of formula (VIc)
And pharmaceutically acceptable salts thereof; wherein R is1And R5As described herein for formula (Ic); n is 0 or 1.
In one embodiment of formula (VIc),
n is 0 or 1;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r 14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl, wherein R is 15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl.
In another embodiment of formula (VIc), n is 0. In another embodiment of formula (VIc), n is 1. In another embodiment of formula (VIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIc), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIc), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIc), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIc), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIc), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIc), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIc), R1Is C (O) NH2. In another embodiment of formula (VIc), R1Is F. In another embodiment of formula (VIc), R 1Is Cl. In another embodiment of formula (VIc), R1Is Br. In another embodiment of formula (VIc), R1Is CN. In another embodiment of formula (VIc), R1Is NH2. In another embodiment of formula (VIc), R1Is NO2. In another embodiment of formula (VIc), R1Is CF3. In another embodiment of formula (VIc), R1Is C (O) OH. In another embodiment of formula (VIc), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds having formula (VIc), including
N- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-phenylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-hydroxy-2-methylpropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (azetidin-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (3S) -pyrrolidin-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-isobutyrylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-benzoylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (methylsulfonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (morpholin-4-yl) cyclopentyl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
Embodiment of formula (VIIc)
In another aspect, the present invention provides a compound of formula (VIIc)
And pharmaceutically acceptable salts thereof; wherein X1、X2、X3And R13As described herein for formula (Ic),represents a single or double bond.
In one embodiment of formula (VIIc),
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
represents a single or double bond;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R6And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r 13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, C1, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl, wherein R is15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (VIIc), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x 1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (VIIc), X1、X2And X3Is CH. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is N. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1. In another embodiment of formula (VIIc), X2Is CH; x1And X3Is N. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is N. In another embodiment of formula (VIIc), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (VIIc), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (VIIc), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (VIIc), X1Is N; x2Is CR1；X3Is N.
In one embodiment of formula (VIIc),is a single bond. In another embodiment of formula (VIIc),is a double bond.
In another embodiment of formula (VIIc), R 1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by one or more groups independently selected from The following groups are substituted: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), R1Is C (O) NH2. In another embodiment of formula (VIIc), R1Is F. In another embodiment of formula (VIIc), R1Is Cl. In another embodiment of formula (VIIc), R1Is Br. In another embodiment of formula (VIIc), R1Is CN. In another embodiment of formula (VIIc), R1Is NH2. In another embodiment of formula (VIIc), R1Is NO2. In another embodiment of formula (VIIc), R1Is CF3. In another embodiment of formula (VIIc), R1Is C (O) OH. In another embodiment of formula (VIIc), R 1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1And X 3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from:R6，OR6，NH2，NHC(O)R6，N(R6)2or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (VIIc), X 1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (VIIc)，X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X 2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkaneOptionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is CF 3. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from And (3) group substitution: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIc), X 1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is NO2. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
Yet another embodiment relates to compounds having formula (VIIc) including
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester;
N- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperidine-1-carboxylic acid tert-butyl ester;
n- [4- (1-butyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-D-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (ethoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-chlorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [3- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (3-thienylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrrol-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2, 5-dimethyl-1H-pyrrol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 3-thiazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3, 5-dimethyl-1, 2-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isonicotinoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (pyridazin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrimidin-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- (4- {1- [3- (piperidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2-hydroxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpiperidin-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (N, N-dimethylglycyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopentylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrrolidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-dioxido-tetrahydro-2H-thiopyran-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methyl-1, 3-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (furan-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -3- (furan-2-yl) prop-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 3-oxazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3, 3, 3-trifluoropropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 5-dimethyl-1H-pyrazol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methoxycyclohexyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2, 3-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-difluorocyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1H-pyrazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tert-butoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-1, 2, 4-triazol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-ethoxypropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-hydroxy-3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-pyrrol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1-methylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methylpropoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1-methyl prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-hydroxycyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1- { [1- (methoxymethyl) cyclopropyl ] carbonyl } -1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (methylsulfonyl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-acetyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -4-methylpent-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-methoxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopent-1-en-1-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (thiophen-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrrol-2-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (4-methylhexanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-dimethylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-5-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclobutylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (piperidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [2- (pyrrolidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
Embodiments of formula (VIIIc)
Accordingly, one embodiment of the present invention is directed to compounds useful as inhibitors of NAMPT having formula (VIIIc), or a pharmaceutically acceptable salt thereof
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R8independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r 12，OR12，SR12，S(O)R12，SO2R12，NHR12，N(R12)2，C(O)R12，C(O)NH2，C(O)NHR12，C(O)N(R12)2，NHC(O)R12，NR12C(O)R12，NHSO2R12，NHC(O)OR12，SO2NH2，SO2NHR12，SO2N(R12)2，NHC(O)NH2，NHC(O)NHR12，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R12independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R12The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more alkoxy groups;
wherein R is3、R6、R8、R10And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r 14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I; wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
R15Independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted with one, two, three or four alkoxy groups;
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In one embodiment of formula (VIIIc), X1、X2And X3Is CH; or X1And X3Is CH; x2Is N; or X1And X3Is CH; x2Is CR1(ii) a Or X2And X3Is CH; x1Is CR1(ii) a Or X1Is CH; x2And X3Is CR1(ii) a Or X2Is CH; x1And X3Is N; or X2And X3Is CH; x1Is N; or X1Is CH; x2Is N; x3Is CR1(ii) a Or X1Is CR1；X2Is N; x3Is CH; or X1Is N; x2Is CR1；X3Is CH; or X1Is N; x2Is CR1；X3Is N. In another embodiment of formula (VIIIc), X1、X2And X3Is CH. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is N. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1. In another embodiment of formula (VIIIc), X1Is CH; x 2And X3Is CR1. In another embodiment of formula (VIIIc), X2Is CH; x1And X3Is N. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is N. In another embodiment of formula (VIIIc), X1Is CH; x2Is N; x3Is CR1. In another embodiment of formula (VIIIc), X1Is CR1；X2Is N; x3Is CH. In another embodiment of formula (VIIIc), X1Is N; x2Is CR1；X3Is CH. In another embodiment of formula (VIIIc), X1Is N; x2Is CR1；X3Is N.
In another embodiment of formula (VIIIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIIc), R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted by one or moreSubstituted with a group independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), R1Is C (O) NH2. In another embodiment of formula (VIIIc), R 1Is F. In another embodiment of formula (VIIIc), R1Is Cl. In another embodiment of formula (VIIIc), R1Is Br. In another embodiment of formula (VIIIc), R1Is CN. In another embodiment of formula (VIIIc), R1Is NH2. In another embodiment of formula (VIIIc), R1Is NO2. In another embodiment of formula (VIIIc), R1Is CF3. In another embodiment of formula (VIIIc), R1Is C (O) OH. In another embodiment of formula (VIIIc), R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heteroA cyclic group; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X 1And X3Is CH; x2Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) NH2. In another embodiment of formula (VIIIc)In scheme (II), X1And X3Is CH; x2Is CR1；R1Is F. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is Cl. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is Br. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is CN. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is NH2. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is NO2. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is CF3. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIIc), X1And X3Is CH; x2Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substitutedSubstituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) NH2. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is F. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is Cl. In another embodiment of formula (VIIIc), X 2And X3Is CH; x1Is CR1；R1Is Br. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is CN. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is NH2. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is NO2. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is CF3. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIIc), X2And X3Is CH; x1Is CR1；R1Is C (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH. In another embodiment of formula (VIIIc), X1Is CH; and X2And X3Is CR1(ii) a And R1Is R3，OR3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH; wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X 1Is CH; x2And X3Is CR1；R1Is R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally independently selected by one or moreSubstituted with a group selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) OR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) NHR3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is NHC (O) R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r 6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is NHSO2R3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; wherein R is6Is an alkyl group or a heterocyclic group. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) NH2. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is F. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is Cl. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is Br. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is CN. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is NH2. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R 1Is NO2. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is CF3. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) OH. In another embodiment of formula (VIIIc), X1Is CH; x2And X3Is CR1；R1Is C (O) R 3(ii) a Wherein R is3Is alkyl, alkenyl or heterocyclyl; wherein each alkyl group is optionally substituted with one or more groups independently selected from: r6，OR6，NH2，NHC(O)R6，N(R6)2Or OH; r6Is an alkyl group or a heterocyclic group.
In one embodiment of formula (VIIIc),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R3independently at each occurrence, is selected from alkyl, alkenyl, or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6OH, F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl or heterocyclyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: f, Cl, Br or I;
R8independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R8Alkyl of (A) or (B)Optionally substituted with one, two, three or four groups independently selected from: r12，OR12OH，CF3F, Cl, Br or I;
R12independently at each occurrence, is selected from alkyl, heterocyclyl or cycloalkyl; wherein each R 12Optionally substituted with one or more alkoxy groups;
wherein R is3、R6、R8And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)NHR13，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SO2R14，NH2，NHR14，N(R14)2，NHC(O)R14，NHC(O)OR14，OH，CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl radicalPyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxy-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl, or cycloalkenyl, optionally substituted with one, two, three, or four groups independently selected from: r 15，OR15，SO2R15，C(O)R15，N(R15)2，NHC(O)R15，OH，CN，CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, OH, F, Cl, Br or I; wherein each R14The aryl, heterocyclyl and cycloalkyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
In another embodiment of formula (VIIIc),
X1、X2and X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
R1Is R3，OR3，C(O)R3，C(O)OR3，C(O)NH2，C(O)NHR3，NHC(O)R3，NHSO2R3，F，Cl，Br，I，CN，NH2，NO2，CF3Or C (O) OH;
R3Independently at each occurrence, is selected from alkyl, alkenyl, or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，NH2，N(R6)2，NHC(O)R6Or OH;
R6independently at each occurrence, is selected from alkyl or heterocyclyl;
R8independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12OH or CF3；
R12Independently at each occurrence, is selected from alkyl, heterocyclyl or cycloalkyl; wherein each R12Optionally substituted with one or more alkoxy groups;
wherein R is3、R6、R8And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SO2R13，C(O)R13，CO(O)R13，NH2，N(R13)2，NHC(O)R13，NHC(O)OR13，C(O)NH2，C(O)NHR13，C(O)N(R13)2，OH，CN，CF3，OCF3，SCF3F or Cl;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R 13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SO2R14，NH2，NHR14，N(R14)2，NHC(O)R14，NHC(O)OR14OH or CF3(ii) a Wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SO2R15，C(O)R15，N(R15)2，NHC(O)R15，CN，OH，CF3F or Cl;
R14independently at each occurrence, is selected from alkyl, aryl, heterocyclyl or cycloalkyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy or OH; wherein each R14The aryl, heterocyclyl and cycloalkyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH or Cl;
R15independently at each occurrence, is selected from alkyl; wherein R is 15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four independently selected alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
Yet another embodiment relates to compounds having formula (VIIic) including
N- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-chlorobenzoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4, 4-difluorocyclohexyl) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (propan-2-yloxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
Pharmaceutical compositions, combination therapy, methods of treatment and administration
Another embodiment includes a pharmaceutical composition comprising a compound of formula (I) and an excipient.
Yet another embodiment includes a method of treating cancer in a mammal, the method comprising: administering to the mammal a therapeutically acceptable amount of a compound of formula (I).
Yet another embodiment relates to a composition for treating a disease during which NAMPT is expressed, said composition comprising an excipient and a therapeutically effective amount of a compound of formula (I).
Yet another embodiment relates to a composition for treating a disease during which ROCK is expressed, said composition comprising an excipient and a therapeutically effective amount of a compound of formula (I).
Yet another embodiment relates to a method of treating a disease in a patient during which NAMPT is expressed, comprising: administering to the patient a therapeutically effective amount of a compound of formula (I).
Yet another embodiment relates to a method of treating a disease in a patient during which ROCK is expressed, comprising: administering to the patient a therapeutically effective amount of a compound of formula (I).
Yet another embodiment relates to a composition for treating: inflammatory and tissue repair disorders; especially rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases, including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, in particular, wherein the cancer is selected from the group consisting of breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatosis, cachexia, inflammation associated with infection and certain viral infections, including acquired immunodeficiency syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia, said composition comprising an excipient and a therapeutically effective amount of a compound of formula (I).
Yet another embodiment relates to a composition for treating: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, dementia of the vascular or AD type, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for preventing graft failure and cystic fibrosis, said composition comprising an excipient and a therapeutically effective amount of a compound of formula (I).
Yet another embodiment relates to a method of treating a patient for: inflammatory and tissue repair disorders; especially rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, in particular, wherein the cancer is selected from the group consisting of breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatosis, cachexia, inflammation associated with infection and certain viral infections including acquired immunodeficiency syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia, comprising: administering to the patient a therapeutically effective amount of a compound of formula (I).
Yet another embodiment relates to a method for treating a patient for: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for preventing graft failure and cystic fibrosis, the method comprising: administering to the patient a therapeutically effective amount of a compound of formula (I).
Yet another embodiment relates to a composition for treating a disease during which NAMPT is expressed, said composition comprising an excipient and a therapeutically effective amount of a compound of formula (I) and a therapeutically effective amount of one other therapeutic agent or more than one other therapeutic agent.
Yet another embodiment relates to a composition for treating a disease during which ROCK is expressed, said composition comprising an excipient and a therapeutically effective amount of a compound of formula (I) and a therapeutically effective amount of one other therapeutic agent or more than one other therapeutic agent.
Yet another embodiment relates to a method of treating a disease in a patient during which NAMPT is expressed, comprising: administering to the patient a therapeutically effective amount of a compound of formula (I) and a therapeutically effective amount of one or more other therapeutic agents.
Yet another embodiment relates to a method of treating a disease in a patient during which ROCK is expressed, comprising: administering to the patient a therapeutically effective amount of a compound of formula (I) and a therapeutically effective amount of one or more other therapeutic agents.
Yet another embodiment relates to a composition for treating: inflammatory and tissue repair disorders; especially rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases, including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, in particular, wherein the cancer is selected from breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatous disease, cachexia, inflammation associated with infection and certain viral infections, including acquired immunodeficiency syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia, the compositions contain an excipient and a therapeutically effective amount of a compound of formula (I) and a therapeutically effective amount of one or more other therapeutic agents.
Yet another embodiment relates to a composition for treating: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, dementia of the vascular or AD type, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct area and myocardial fibrosis, for preventing graft failure and cystic fibrosis, said composition containing an excipient and a therapeutically effective amount of a compound of formula (I) and a therapeutically effective amount of one or more other therapeutic agents.
Yet another embodiment relates to a method of treating a patient for: inflammatory and tissue repair disorders; especially rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, in particular, wherein the cancer is selected from the group consisting of breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatosis, cachexia, inflammation associated with infection and certain viral infections including acquired immunodeficiency syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia, comprising: administering to the patient a therapeutically effective amount of a compound of formula (I) and a therapeutically effective amount of one or more other therapeutic agents.
Yet another embodiment relates to a method for treating a patient for: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for preventing graft failure and cystic fibrosis, the method comprising: administering to the patient a therapeutically effective amount of a compound of formula (I) and a therapeutically effective amount of one or more other therapeutic agents.
Metabolites of the compounds of formula (I) produced by metabolic processes in vitro or in vivo may also be useful in the treatment of NAMPT-related diseases.
Metabolites of the compounds of formula (I) produced by metabolic processes in vitro or in vivo may also be useful in the treatment of ROCK-related diseases.
Certain precursor compounds that can be metabolized in vitro or in vivo to form compounds of formula (I) may also be useful in the treatment of diseases associated with NAMPT.
Certain precursor compounds that can be metabolized in vitro or in vivo to form compounds of formula (I) may also be useful in the treatment of ROCK-associated diseases.
The compounds of formula (I) may exist in the form of acid addition salts, base addition salts or zwitterions. Salts of the compounds are prepared during isolation of the compounds or after purification of the compounds. Acid addition salts of compounds are those salts obtained by reacting a compound with an acid. For example, the present invention is intended to include the acetate, adipate, alginate, bicarbonate, citrate, aspartate, benzoate, benzenesulfonate, bisulfate, butyrate, camphorate, camphorsulfonate, digluconate, formate, fumarate, glycerophosphate, glutamate, hemisulfate, heptanoate, hexanoate, hydrochloride, hydrobromide, hydroiodide, lactobionate, lactate, maleate, mesitylenesulfonate, methanesulfonate, naphthalenesulfonate, nicotinate, oxalate, pamoate, pectinate, persulfate, phosphate, picrate, propionate, succinate, tartrate, thiocyanate, trichloroacetate, trifluoroacetate, p-toluenesulfonate and undecanoate salts of the compounds. Base addition salts of compounds are those obtained by reacting a compound with a hydroxide, carbonate or bicarbonate of a cation, such as lithium, sodium, potassium, calcium and magnesium.
The compounds of formula (I) may be administered in the following manner: for example, buccal, ocular, oral, osmotic, parenteral (intramuscular, intraperitoneal, intrasternal, intravenous, subcutaneous), rectal, topical, transdermal or vaginal.
A therapeutically effective amount of a compound of formula (I) will depend upon the recipient of the treatment, the condition being treated and its severity, the composition containing the compound, the time of administration, the route of administration, the duration of the treatment, the potency of the compound, its clearance rate and whether it is co-administered with another drug. The amount of a compound of formula (I) of the present invention used to prepare a composition for daily administration to a patient in a single dose or in divided doses is from about 0.03 to about 200mg/kg body weight. Single dose compositions contain these amounts or a combination of sub amounts (submultiple) thereof.
The compounds of formula (I) may be administered with or without excipients. Excipients include, for example, encapsulating materials and additives such as absorption promoters, antioxidants, binders, buffers, coating agents, colorants, diluents, disintegrants, emulsifiers, bulking agents, fillers, flavoring agents, humectants, lubricants, flavorants, preservatives, propellants, detackifiers, bactericides, sweeteners, solubilizers, wetting agents and mixtures thereof.
Excipients for the preparation of compositions containing compounds of formula (I) for oral administration in solid dosage form include, for example, agar, alginic acid, aluminium hydroxide, benzyl alcohol, benzyl benzoate, 1, 3-butylene glycol, carbomer, castor oil, cellulose acetate, cocoa butter, corn starch, corn oil, cottonseed oil, crospovidone, diglycerides, ethanol, ethylcellulose, ethyl laurate, ethyl oleate, fatty acid esters, gelatin, germ oil, glucose, glycerol, peanut oil, hydroxypropyl methylcellulose, isopropanol, isotonic saline, lactose, magnesium hydroxide, magnesium stearate, maltol, mannitol, monoglycerides, olive oil, peanut oil, potassium phosphate salts, potato starch, povidone, propylene glycol, ringer's solution, safflower oil, sesame oil, sodium carboxymethylcellulose, sodium phosphate salts, sodium lauryl sulfate, sodium sorbitol, soybean oil, stearic acid, stearyl fumarate, sucrose, surfactants, talc, tragacanth, tetrahydrofurfuryl alcohol, triglycerides, water, and mixtures thereof. Excipients for preparing liquid dosage forms for ocular or oral administration of compositions containing a compound of formula (I) of the present invention include, for example, 1, 3-butylene glycol, castor oil, corn oil, cottonseed oil, ethanol, fatty acid esters of sorbitan, germ oil, peanut oil, glycerol, isopropanol, olive oil, polyethylene glycol, propylene glycol, sesame oil, water and mixtures thereof. Excipients useful in preparing compositions containing compounds of formula (I) of the present invention for osmotic administration include, for example, chlorofluorocarbons, ethanol, water and mixtures thereof. Excipients useful in preparing compositions containing compounds of formula (I) of the present invention for parenteral administration include, for example, 1, 3-butylene glycol, castor oil, corn oil, cottonseed oil, glucose, germ oil, peanut oil, liposomes, oleic acid, olive oil, peanut oil, ringer's solution, safflower oil, sesame oil, soybean oil, u.s.p. or isotonic sodium chloride solution, water and mixtures thereof. Excipients useful in preparing compositions containing compounds of formula (I) of the present invention for rectal or vaginal administration include, for example, cocoa butter, polyethylene glycols, waxes and mixtures thereof.
The compounds of formula (I) are expected to be effective when used together with: alkylating agents, angiogenesis inhibitors, antibodies, metabolic antagonists, antimitotic agents, antiproliferative agents, antiviral agents, aurora kinase inhibitors, other apoptosis promoters (e.g., Bcl-xL, Bcl-w, and Bfl-1 inhibitors), activators of death receptor pathways, Bcr-Abl kinase inhibitors, BiTE (bispecific T-cell engager) antibodies, antibody-drug conjugates, biological response modifiers, cyclin-dependent kinase inhibitors, cell cycle inhibitors, cyclooxygenase-2 inhibitors, DVDs, ErbB leukemia virus oncogene homolog (2) receptor inhibitors, growth factor inhibitors, Heat Shock Protein (HSP) -90 inhibitors, Histone Deacetylase (HDAC) inhibitors, hormone therapy, immunity, Inhibitors of Apoptosis Proteins (IAPs), intercalating antibiotics, kinase inhibitors, kinesin inhibitors, Jak2 inhibitors, mammalian-targeted rapamycin inhibitors, microRNAs, mitogen-activated extracellular signal-regulated kinase inhibitors, multivalent binding proteins, non-steroidal anti-inflammatory drugs (NSAIDs), poly-ADP (adenosine diphosphate) -ribose polymerase (PARP) inhibitors, platinum chemotherapeutic drugs, polo-like kinase (Plk) inhibitors, phosphoinositide-3 kinase (PI3K) inhibitors, proteosome inhibitors, purine analogs, pyrimidine analogs, receptor tyrosine kinase inhibitors, retinoid/poplar (deltoids) plant alkaloids, small molecule inhibitory ribonucleic acid (siRNAs), topoisomerase inhibitors, ubiquitin ligase inhibitors, and the like, and forms of one or more of these agents.
BiTE is a bispecific antibody that directs T cells to attack cancer cells by binding to both cells simultaneously. The T cells then attack the targeted cancer cells. Examples of BiTE antibodies include: adermumab (ademight) (Micromet MT201), blinatumomab (Micromet MT103), and the like. Without being limited by theory, the mechanism by which T cells cause apoptosis of targeted cancer cells is by exocytosis of cytolytic granule components, which include perforin and granzyme B. In this regard, Bcl-2 has been shown to attenuate both perforin and granzyme B induced apoptosis. These data suggest that inhibition of Bcl-2 can increase the cytotoxic effects caused by T cells when targeting cancer cells (v.r. sutton, d.l.vaux and j.a. trapani, j.of immunology 1997, 158(12), 5783).
SiRNAs are molecules with endogenous RNA bases or chemically modified nucleotides. The modification does not abrogate cellular activity, but confers increased stability and/or increases the potency of the cell. Examples of chemical modifications include phosphorothioate groups, 2 '-deoxynucleotides, nucleotides containing 2' -OCH3-, 2 '-F-nucleotides, 2' -methoxyethyl nucleotides, combinations thereof, and the like. sirnas can have varying lengths (e.g., 10-200bps) and structures (e.g., hairpins, single/double strands, protrusions, notch/notch chromosomes, dislocations) and are processed in cells to provide active gene silencing. Double-stranded sirna (dsrna) has the same number of nucleotides on each strand (blunt end) or asymmetric end (overhang). Overhangs of 1-2 nucleotides may be present on the sense and/or antisense strand, as well as on the 5 '-and/or 3' -end of a given strand.
Multivalent binding proteins are binding proteins that include two or more antigen binding sites. Multivalent binding proteins can be engineered to have three or more antigens, which are typically naturally occurring antibodies. The term "multispecific binding protein" refers to a binding protein capable of binding two or more related or unrelated targets. Dual Variable Domain (DVD) binding proteins are tetravalent or multivalent binding proteins that include two or more antigen binding sites. Such DVDs can be monospecific (i.e., capable of binding one antigen) or multispecific (i.e., capable of binding two or more antigens). DVD binding proteins comprising two heavy chain DVD polypeptides and two light chain DVD polypeptides are referred to as DVD Ig's. Each half of the DVD Ig includes one heavy chain DVD polypeptide, one light chain DVD polypeptide, and two antigen binding sites. Each binding site includes a heavy chain variable domain and a light chain variable domain, and each antigen binding site has a total of 6 CDRs involved in antigen binding.
Alkylating agents include altretamine, AMD-473, AP-5280, apaziquone, bendamustine, brositallicin, busulfan, carboquone, carmustine (BCNU), chlorambucil,(lamotrigine, VNP 40101M), cyclophosphamide, deschloroxazine, estramustine, fotemustine, glufosfamide, ifosfamide, KW-2170, lomustine (CCNU), macsfamide (mafosfamide), melphalan, dibromomannitol, dibromodulcitol, pyrimidine nitrosourea, nitrogen mustard N-oxide, Ranimustine (Ranimustine), temozolomide, thiotepa, (bendamustine), troosulfan, chloroacetohydrofamide, and the like.
Angiogenesis inhibitors include: endothelial-specific receptor tyrosine kinase (Tie-2) inhibitors, Epidermal Growth Factor Receptor (EGFR) inhibitors, insulin growth factor-2 receptor (IGFR-2) inhibitors, matrix metalloproteinase-2 (MMP-2) inhibitors, matrix metalloproteinase-9 (MMP-9) inhibitors, platelet growth factor receptor (PDGFR) inhibitors, thrombospondin analogs, vascular endothelial growth factor receptor tyrosine kinase (VEGFR) inhibitors, and the like.
The metabolic antagonist comprises(disodium Pemetrexed, LY231514, MTA), 5-azacitidine,(capecitabine), carmofur,(cladribine), clofarabine, cytarabine sodium octadecylphosphate, cytosine arabinoside, decitabine, deferoxamine, doxifluridine, eflornithine, EICAR (5-ethynyl-1- β -D-ribofuranosylimide zole-4-carboxamide), enocitabine, ethnylcytidine, fludarabine, 5-fluorouracil alone or in combination with folinic acid,(Jixita)Shore), a hydroxyurea,(melphalan), mercaptopurine, 6-mercaptopurine ribonucleosides, methotrexate, mycophenolic acid, nelarabine (nelarabine), nolatrexed (nolatrexed), sodium octadecylphosphate, pyritrexol (pellitrexol), pentostatin, raltitrexed (raltitrexed), ribavirin, triapine, trimetrexate, S-1, thiazolofuran, tegafur, TS-1, vidarabine, UFT and the like.
Antiviral agents include ritonavir, hydroxychloroquine, and the like.
Aurora kinase inhibitors include ABT-348, AZD-1152, MLN-8054, VX-680, aurora A-specific kinase inhibitors, aurora B-specific kinase inhibitors and panaurora kinase inhibitors, and the like.
Bcl-2 protein inhibitors include: AT-101((-) gossypol),(G3139 or Olimersen) (Bcl-2-targeting antisense oligonucleotide)), IPI-194, IPI-565, N- (4- (4- ((4 '-chloro (1, 1' -biphenyl) -2-yl) methyl) piperazin-1-yl) benzoyl) -4- (((1R) -3- (dimethylamino) -1- ((phenylsulfanyl) methyl) propyl) amino) -3-nitrobenzenesulfonamide) (ABT-737), N- (4- (4- ((2- (4-chlorophenyl) -5, 5-dimethyl-1-cyclohex-1-en-1-yl) methyl) piperazin-1-yl) benzoyl) -4- (((1R) -3- (morpholin-4-yl) benzoyl) -3-nitrobenzenesulfonamide -yl) -1- ((phenylsulfanyl) methyl) propyl) amino) -3- ((trifluoromethyl) sulfonyl) benzenesulfonamide (ABT-263), GX-070(obatoclax), and the like.
Bcr-Abl kinase inhibitors include:(BMS-354825)，(imatinib), and the like.
CDK inhibitors include: AZD-5438, BMI-1040, BMS-032, BMS-387, CVT-2584, Frataxidol (flavopiridol), GPC-286199, MCS-5A, PD0332991, PHA-690509, seliciclib (CYC-202, R-roscovitine), ZK-304709, and the like.
COX-2 inhibitors include: the ABT-963 is used for the anti-tumor drug delivery system,(etoricoxib) is added to the mixture,(valdecoxib), BMS347070,(celecoxib), COX-189 (lumiracoxib), CT-3,(deracoxib), JTE-522, 4-methyl-2- (3, 4-dimethylphenyl) -1- (4-sulfamoylphenyl-1H-pyrrole), MK-663 (etoricoxib), NS-398, parecoxib, RS-57067, SC-58125, SD-8381, SVT-2016, S-2474, T-614,(rofecoxib), and the like.
EGFR inhibitors include: ABX-EGF, anti-EGFR immunoliposome, EGF-vaccine, EMD-7200,(cetuximab), HR3, IgA antibodies,(gefitinib) is added to the composition,(erlotinib or OSI-774), TP-38, EGFR fusion protein,(lapatinib: (lapatinib)), and the like.
ErbB2 receptor inhibitors include: CP-724-714, CI-1033 (caritinib),(trastuzumab),(lapatinib),(2C4, pertuzumab (pertuzumab)), TAK-165, GW-572016 (ionofanib), GW-282974, EKB-569, PI-166, dHER2(HER2 vaccine), APC-8024(HER-2 vaccine), anti-HER/2 neu bispecific antibody, B7.HER2IgG3, AS HER2 trifunctional bispecific antibody, mAB AR-209, mAB 2B-1, and the like.
Histone deacetylase inhibitors include: depsipeptides, LAQ-824, MS-275, tropicin (trapoxin), suberoylanilide hydroxamic acid (SAHA), TSA, valproic acid and the like.
HSP-90 inhibitors include: 17-AAG-nab, 17-AAG, CNF-101, CNF-1010, CNF-2024, 17-DMAG, geldanamycin, IPI-504, KOS-953,(human recombinant antibody of HSP-90), NCS-683664, PU24FCl, PU-3, radicicol, SNX-2112, STA-9090 VER49009, and the like.
Inhibitors of apoptosis proteins include: HGS1029, GDC-0145, GDC-0152, LCL-161, LBW-242, and the like.
Antibody-drug conjugates include: anti-CD 22-MC-MMAF, anti-CD 22-MC-MMAE, anti-CD 22-MCC-DM1, CR-011-vcMAE, PSMA-ADC, MEDI-547, SGN-19Am SGN-35, SGN-75, and the like.
Activators of the death receptor pathway include: TRAIL, antibodies targeting TRAIL or death receptors (e.g. DR4 and DR5) or other agents such as Apomab, conatumumab, ETR2-ST01, GDC0145 (lexatumumab), HGS-1029, LBY-135, PRO-1762 and trastuzumab.
Kinesin inhibitors include: eg5 inhibitors, such as AZD4877, ARRY-520; CENPE inhibitors, such as GSK923295A and the like.
JAK-2 inhibitors include: CEP-701 (lesauritinib), XL019, and INCB018424, and the like.
MEK inhibitors include: ARRY-142886, ARRY-438162, PD-325901, PD-98059, and the like.
mTOR inhibitors include: AP-23573, CCI-779, everolimus, RAD-001, rapamycin, sirolimus (temsirolimus), ATP competitive TORC1Inhibitors of/TORC 2, including PI-103, PP242, PP30, Torin 1, and the like.
Non-steroidal anti-inflammatory drugs include:(bis-salicyl ester),(diflunisal) is added to the mixture,(ibuprofen) is added to the reaction mixture,(ketoprofen),(nabumetone) is added to the mixture,(piroxicam), ibuprofen cream,(naproxen) and(naproxen) is added to the solution,(diclofenac acid) and (C) in a solvent,(anti-inflammatory pain),(sulindac) is added to the mixture,(toluoylpipecolic acid),(the presence of etodolac),(ketorolac) is added to the aqueous solution,(oxaprozin), and the like.
PDGFR inhibitors include: c-451, CP-673, CP-868596, and the like.
Platinum chemotherapeutic agents include: the cisplatin (cisplatin) is used as a raw material,(oxaliplatin), eptaplatin, ledaplatin, nedaplatin,(carboplatin), satraplatin, picoplatin, and the like.
Inhibitors of the equine (Polo-like) kinase include BI-2536 and the like.
Phosphoinositide-3 kinase (PI3K) inhibitors include: wortmannin, LY294002, XL-147, CAL-120, ONC-21, AEZS-127, ETP-45658, PX-866, GDC-0941, BGT226, BEZ235, XL765 and the like.
Thromboxane analogs include: ABT-510, ABT-567, ABT-898, TSP-1, and the like.
VEGFR inhibitors include: (bevacizumab), ABT-869, AEE-788, ANGIOZYMETM(angiostatic ribozymes (Boulder, CO.) and Chiron (Emeryville, CA)), Asitinib (AG-13736), AZD-2171, CP-547, 632, IM-862, MACUGEN (pegaptanib)),(sorafenib, BAY43-9006), pazopanib (pazopanib) (GW-786034), vatalanib (vatalanib) (PTK-787, ZK-222584),(Sunitinib, SU-11248), VEGF trap, ZACTIMATM(vandetanib), ZD-6474) and the like.
The antibiotics include: insertion of antibiotics, such as doxorubicin, actinomycin D, amrubicin, anthracycline (annamycin), doxorubicin,(bleomycin), daunorubicin,or(liposomal doxorubicin), elsamitrucin, epirubicin (epirubicin), glarbuiin,(idarubicin), mitomycin C, nemorubicin, neocarzinostatin, pellomycin sulfate, pirarubicin, rebeccamycin, netastatin (stimamer), streptoverticilliumThe content of the element is as follows,(valrubicin), neocarzinostatin, and the like.
Topoisomerase inhibitors include: aclarubicin, 9-aminocamptothecin, amnafide, amsacrine, bicatecarin, belotecan (belotecan), BN-80915, (irinotecan hydrochloride), camptothecin,(dexpropinine), difluotecan (diflomotecan), Dudidibucalin (edotecarin),or(epirubicin), etoposide, irinotecan (exatecan), 10-hydroxycamptothecin, gemmacetan, lurotecan, mitoxantrone, rubitecan (orathecin), pirarubicin (pirarubicin), pixantrone (pixantrone), rubitecan, sobuzosin, SN-38, afluposide, topotecan, and the like.
The antibody comprises:(bevacizumab), CD 40-specific antibody, chTNT-1/B, denosumab (denosumab),(cetuximab) and (c) in the presence of a pharmaceutically acceptable carrier,(zanolimumab), IGF 1R-specific antibodies, lintuzumab,(ibritumomab) in a pharmaceutically acceptable carrier,(WX G250)，(rituximab), ticalimumab, trastuzimab, type I and type II CD20 antibodies, and the like.
Hormone therapy includes:(anastrozole) is added to the mixture,(exemestane), azoxifene,(bicalutamide) and (ii) a salt thereof,(cetrorelix), degareleix, deslorelin,(trilostane), dexamethasone, and combinations thereof,(the amount of flutamide),(Ranoxiphenol), AFEMAMOMUM (fadrozole),(toremifene),(fulvestrant) is added to the composition,(letrozole), formestane, sugarA corticosteroid is a substance that is capable of inducing the onset of an inflammatory response,(doxercalciferol), (sevelamer carbonate), lasofoxifene, leuprolide acetate,(megestrol) and (I),(mepiquat chloride), NILANDRONTM (nilutamide),(tamoxifen citrate), PLENAXISTM(aberralix), dehydrocortisone,(finasteride), rilostate,(buserelin) in a pharmaceutically acceptable carrier,(luteinizing hormone releasing hormone (LHRH)),(histrelin implants),(trilostane or modastane),(fosrelin, goserelin) and the like.
Deltoids and retinoids include: seocalcitol () (EB1089, CB1093), lexacalcitol (KH1060), fennelTretinoin (fenretinide),(aliretinoin)，(the liposome of retinoic acid),(bexarotene), LGD-1550, and the like.
PARP inhibitors include: ABT-888(veliparib), olaparib (olaparib), KU-59436, AZD-2281, AG-014699, BSI-201, BGP-15, INO-1001, ONO-2231 and the like.
Plant alkaloids include, but are not limited to: vincristine, vinblastine, desacetylvinblastine, vinorelbine, and the like.
Proteasome inhibitors include:(bortezomib), MG132, NPI-0052, PR-171, and the like.
Examples of immunological agents include interferon and other immune-enhancing agents. The interferon includes: interferon alpha, interferon alpha-2 a, interferon alpha-2 b, interferon beta, interferon gamma-1 a, (interferon γ -1b), interferon γ -n1, combinations thereof, and the like. Other agents include:(IFN-. alpha.), BAM-002 (oxidized glutathione),(tasonermin),(tositumomab)),(alemtuzumab), CTLA4 (cytotoxic lymphocyte antigen 4), dechlorohydroxazine, denine interleukin (denileukin), epratuzumab,(leguminoxane), lentinan, leukocyte interferon-alpha, imiquimod, MDX-010 (anti-CTLA-4), melanoma vaccine, mitumomab, moraxepin, MYLOTARGTM(gemtuzumab ozogamicin (gemtuzumab)),(filgrastim), OncoVAC-CL,(agovomab (oregovmamab)), pemtumumab (Y-muHMFG 1),(sipuleucel-T), sargaramostim, xizopyran, TexelInterleukin (teceleukin),(Bacillus Calmette-Guerin), ubenimex,(immunotherapeutic agents, Lorus Pharmaceuticals), Z-100 (Maruyama's Specific Substance (SSM)), WF-10 (Tetrachlorodecaoxide (TCDO)),(aldesleukin),(thymalfasin),(daclizumab),(90Y-ibritumomab tiuxetan), and the like.
Biological response modifiers are agents that improve the defense mechanism or biological response of the organism, such as survival, growth or differentiation of tissue cells, rendering them antitumor, including coriolus versicolor polysaccharide k (krestin), lentinan, cezopyran, streptolysin (picibanil), PF-3512676(CpG-8954), ubenimex, and the like.
Pyrimidine analogs include: cytarabine (ara C or arabinoside C), cytosine arabinoside, doxifluridine,(fludarabine), 5-FU (5-fluorouracil), azauridine,(gemcitabine), in the presence of a carrier gas,(ratitrexed)，TROXATYLTM(triacetyluridine troxacitabine (troxacitabine)), and the like. Purine analogs include:(thioguanine) and(mercaptopurine).
Anti-mitotic agents include: barbitulin (batabulin), epothilone D (KOS-862), N- (2- ((4-hydroxyphenyl) amino) pyridin-3-yl) -4-methoxybenzenesulfonamide, ixabepilone (ixabepilone) (BMS 247550), paclitaxel,(docetaxel), PNU100940(109881), ixabepilone (patupilone), XRP-9881 (larotaxel), vinflunine, ZK-EPO (synthetic epothilone), and the like.
Ubiquitin ligase inhibitors include: MDM2 inhibitors, such as nutlins, NEDD8 inhibitors, such as MLN4924, and the like.
The compounds of the invention may also be used as radiosensitizers to enhance the effectiveness of radiotherapy. Examples of radiotherapy include: external beam radiation therapy, deep treatment, superficial treatment and sealed source, unsealed source radiation therapy, and the like.
In addition, the compounds of formula (I) may be combined with other chemotherapeutic agents, e.g., ABRAXANETM(ABI-007), ABT-100 (farnesyl transferase inhibitor),(Ad5CMV-p53 vaccine),or(lovastatin) in a liquid medium,(poly I-poly C12U, synthetic RNA),(Exisulin (exisulind)),(pamidronic acid), arglabin, levoasparaginase, atamestan (1-methyl-3, 17-dione-androstane-1, 4-diene),(tretinoin (tazarotene)), AVE-8062 (combretastatin derivative), BEC2 (mitumomab), cachectin or cachexin (tumor necrosis factor), canvaxin (a vaccine),(cancer vaccine),(the western-Mol interleukin) protein,(the dihydrochloride group is shown in the specification),(human papillomavirus vaccine),(C：(cyclophosphamide) H:(hydroxydoxorubicin); o: vincristineP: dehydrocortisone), CYPATTM(Seslolone acetate), combestina 4P, DAB (389) EGF (catalytic and migratory domain of diphtheria toxin fused to human epidermal growth factor via His-Ala linker) or TransMID-107R TM(diphtheria toxin), dacarbazine, actinomycin, 5, 6-dimethylxanthenone-4-acetic acid (DMXAA), eniluracil, EVIZONTM(squalamine lactate),(T4N5 Liposomal lotion), discodermolide, DX-8951f (Exatecan mesylate), enzastaurin, EPO906(epithilone B)(tetravalent human papilloma virus (6, 11, 16, 18 types) recombinant vaccine),GMK (ganglioside conjugate vaccine),(prostate cancer vaccine), halofuginone (halofuginone), histerelin (histerelin), hydroxyurea, ibandronic acid, IGN-101, IL-13-PE38, IL-13-PE38QQR (cindrekin bestotox), IL-13-Pseudomonas exotoxin, interferon-alpha, interferon-gamma, JUNOVANTMOr MEPACTTM(mivampide), lonafarnib, 5, 10-methylenetetrahydrofolic acid, miltefosine (hexadecylphosphocholine),(AE-941)，(tritrexate glucuronate),(pentostatin),(ribonuclease),(melanoma vaccine therapy),(IL-2 vaccine), ORATHECINTM(rubitecan) which is a drug substance,(antibody-based cellular pharmaceuticals),MAb (murine monoclonal antibody), paclitaxel, PANDIMEXTM(aglycone sapogenins derived from Ginseng radix, including 20(S) -protopanaxas radix Terpineol (aPPD) and 20(S) -protopanaxatriol (aPPT)), panitumumab (panitumumab),VF (investigated cancer vaccine), pegapase, PEGylated interferon A, phenoxadiol, procarbazine, remamastat,(catumaxomab)，(lenalidomide), RSR13 (efaproxiral),LA (a peptide of lanreotide),(Avermectin), staurosporine (Streptomyces stellate spores), talabostat (PT 100),(bexarotene),(DHA-paclitaxel),(canfosfamide，TLK286)，temilifene，(temozolomide), telmisilifene (tesmilifene), reaction was stopped,(STn-KLH), thymitaq (2-amino-3, 4-dihydro-6-methyl-4-oxo-5- (4-pyridylthio) quinazoline dihydrochloride), TNFaradETM(adenovirus vector: DNA vector containing tumor necrosis factor-alpha Gene)，Or(bosentan), tretinoin (Retin-A), tetrandrine,(arsenic trioxide),ukrain (alkaloid derivatives of celandine plants), vitaxin (anti-alphavbeta 3 antibody),(motexfin) gadolinium, XINLAYTM(atrasentan), XYOTAXTM(paclitaxel poliglumex)),(trabectedin), ZD-6126,(dexrazoxane) in the presence of a pharmaceutically acceptable carrier, (zoledronic acid), zorubicin, and the like.
Data of
The utility of the compounds of formula (I) as binding agents and inhibitors of NAMPT was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) binding assay.
Time-resolved fluorescence resonance energy transfer (TR-FRET) binding assay for NAMPT
In 18. mu.L low-volume plates (Owens Corning) in reaction buffer (50mM HEPES (NaOH)), pH7.5, 100mM NaCl, 10mM MgCl21mM DTT, 1% glycerol) was performedFor assay, 6.8nM recombinant human C-terminal His-tagged NAMPT, 1nM Tb-anti-His antibody (Invitrogen, Cat # PV5895), and 200nM probe (Oregon Green 488-conjugated APO 866; A-1251667.0 (Probe 1) or A-1287128.0 (Probe 2)) were used. The plate was covered and the reaction was allowed to proceed for 2-3 hours. After 2 to 3 hours, plates were read using Envision (Laser Lantha low volume protocol). Excitation at 337nm, the emission ratio of Oregon Green (520nm) to Terbium (492nm) was determined and used to calculate the IC of the test compound50The value is obtained.
Table 1 shows the utility of the compounds of formula I for functional inhibition of NAMPT.
TABLE 1
nd is not measured.
ROCK2 kinase Activity assay
[ 33 P]-ATP assay:ROCK2 activity was initially determined using a radioactive flash plate-based assay. In a 96-well plate, a biotinylated peptide substrate (final 2. mu.M; abbreviation of S6-ROCK 2), γ -, [ alpha ], [ 33P]ATP (5. mu.M, 2 mCi/. mu.mol), compound (0.1-10000nM in 2% DMSO) and ROCK2(0.2 nM; Upstate) catalytic domain.
HTRF test:the assay used the CisBio HTRF KinEASE kit (kit 62ST2PEZ) and the kinase reaction contained the same as above33P-ATP assay-identical 0.2. mu.M biotinylated substrate peptide (S2, CisBio), 5. mu.M, 100. mu.M or 1mM ATP, inhibitor (0.1-10,000 nM in 2% DMSO) and enzyme.
Table 2 shows the results of the HTRF test and the utility of the compounds of formula I for their functional inhibition of ROCK 2.
TABLE 2
nd is not measured.
Compounds that inhibit NAMPT are useful for treating diseases involving the activation of NF-KB. Such methods are useful for treating a variety of diseases, including, inflammatory and tissue repair disorders; especially rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases, including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, in particular, wherein the cancer is selected from the group consisting of breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatosis, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia.
WO 97/48696 describes the relationship to NAMPT in the treatment of cancer. WO97/48397 describes the relationship of immunosuppression to NAMPT. WO 2003/80054 describes the relationship of treatment of diseases involving angiogenesis to NAMPT. WO 2008/025857 describes the treatment of rheumatoid arthritis and septic shock in relation to NAMPT. WO 2009/109610 describes the prevention and treatment of ischemia in relation to NAMPT.
Cancers include, but are not limited to: hematological and solid tumor types, such as acoustic neuroma, acute leukemia, acute lymphoblastic leukemia, acute myeloid leukemia (monocytes, myeloblasts, adenocarcinomas, angiosarcomas, astrocytomas, myelomonocytes and promyelocytes), acute T-cell leukemia, basal cell carcinoma, bile duct carcinoma, bladder carcinoma, brain cancer, breast cancer (including estrogen-receptor positive breast cancer), bronchial cancer, Burkitt's tumor, cervical cancer, chondrosarcoma, chordoma, choriocarcinoma, chronic leukemia, chronic lymphocytic leukemia, chronic myeloid (granulocytic) leukemia, chronic myelogenous leukemia, colon cancer, colorectal cancer, craniopharyngioma, cystadenocarcinoma, proliferative changes (dysplasia and tissue deformation), embryonal cancer, endometrial cancer, endotheliosarcoma, ependymoma, epithelial cancer, erythroleukemia, esophageal cancer, estrogen-receptor positive breast cancer, essential thrombocythemia, ewing's tumor, fibroma Retinoblastoma, gastric carcinoma, germ cell testicular carcinoma, gestational trophoblastic disease, glioblastoma, head and neck carcinoma, heavy chain disease, hemangioblastoma, liver carcinoma, hepatocellular carcinoma, hormone-insensitive prostate carcinoma, leiomyosarcoma, liposarcoma, lung carcinoma (including small cell lung carcinoma and non-small cell lung carcinoma), lymphatic endothelial sarcoma, lymphatic sarcoma, lymphocytic leukemia, lymphoma (lymphoma, including diffuse large B-cell lymphoma, follicular lymphoma, hodgkin's lymphoma and non-hodgkin's lymphoma), malignant tumors and hyperproliferative disorders of the bladder, breast, colon, lung, ovary, pancreas, prostate, skin and uterus, lymphoid malignancies of T-cell or B-cell origin, leukemia, myeloid carcinoma, medulloblastoma, melanoma, meningioma, mesothelioma, multiple myeloma, granulocytic leukemia, myeloma, myxosarcoma, neuroblastoma, oligodendroglioma, oral cancer, osteogenic sarcoma, ovarian cancer, pancreatic cancer, papillary adenocarcinoma, papillary carcinoma, peripheral T-cell lymphoma, pinealoma, polycythemia vera, prostate cancer (including hormone-insensitive (refractory) prostate cancer), rectal cancer, renal cell carcinoma, retinoblastoma, rhabdomyosarcoma, sarcoma, sebaceous gland carcinoma, seminoma, skin cancer, small cell lung cancer, solid tumors (carcinomas and sarcomas), gastric cancer, squamous cell carcinoma, synovioma, sweat gland carcinoma, testicular cancer (including germ cell testicular cancer), thyroid cancer, Macroglobulinemia, testicular tumor, uterine cancer, Wilms' tumor, and the like.
Aberrant activation of the Rho/ROCK pathway has been observed in a variety of disorders (Wettschureck, N., Offermanns, S., Rho/Rho-kinase media signaling in physiology and pathobiology. J. mol. Med.80, 2002, 629 638; Muller, B.K., Mack, H., Teusch, N., Rho kinase, amplifying driver target for neurological disorders, Nat. Dr. Discov. 4, 2005, 387 398; Hu, E, Lee, D., ROCK inhibitors potential therapeutic agents for car cancer)ovesicular diseases, curr, opin, investig, drugs, 4, 2003, 1065-. As already stated, ROCKs phosphorylate myosin binding to a subtype of Myosin Light Chain (MLC) phosphatase (MLCP), increasing myosin phosphorylation and actin-myosin contractility (Somlyo, A.P., Somlyo, A.V., Ca2+ sensitivity of smooth and nonmuslemycin II: modulated by G proteins, kinases, and myostatin phosphor. physiology. Rev.83, 2003, 1325-. Examples of disease states associated with aberrant Rho/ROCK activity (particularly vasospastic activity) include: cardiovascular diseases, such as hypertension (Satoh S., Kreutz R., Wilm C., Ganten D., Pfitzer G., Austelegadoist-induced Ca) 2+-a localization of a nuclear area transformation of an interactive scientific great rates. evaluation for an altered signal transmission of nuclear small cells. J. Clin. invest.94, 1994, 1397-1403; mukai, y., Shimokawa, h., Matoba, t., Kandabashi, t., Satoh, s., Hiroki, j., Kaibuchi, k., Takeshita, a., invasion of Rho-kinase in hyper vascular disease: a novel therapeutic target in hyper tension. FASEB J.15, 2001, 1062-1064; uehata, m., Ishizaki, t., Satoh, h., Ono, t., Kawahara, t., Morishita, t., Tamakawa, h., Yamagami, k., Inui, j., Maekawa, m., Narumiya, s., Calcium sensing of smooth muscle conditioned by a Rho-associated protein kinase in hypertension. nature389, 1997, 990-; masumoto, A., Hirooka, Y., Shimokawa, H., Hironaga, K., Setoguchi, S., Takeshita, A., Possibleinvolvent of Rhokinase in The patient diagnosis of hypertension in humans hyper tension 38, 2001, 1307-; shimokawa, H., Cellular and molecular industries of coronary artery spasm: lessons from animal models. JpnCirc J64, 2000, 1-12; Shimokawa, h., Morishige, k., Miyata, k., Kandabashi, t., Eto, y., Ikegaki, i., Asano, t., Kaibuchi, k., Takeshita, a., Longterm inhibition of Rho-kinase activities alignment of aqueous coronar dispersions in a porous model in vivo.cardio Res 51, 2001, 169 one 177; utsunomiya, t., Satoh, s., Ikegaki, i., Toshima, y, Asano, t, Shimokawa, h., antibodies of hydroxyfacial tissue, a Rho-kinase inhibitor, in a kinase model of expression and br J Pharmacol 134, 201, 1724-; sah, v.p., Hoshijima, m., Chien, k.r., Brown, j.h., Rho required for Galphaq and alpha 1-acquired receiver signal-637 for acquiring in cardio cells, diagnosis of Ras and Rho pathways.j Biol Chem271, 1996, 31185-one 1190; kuwahara, k., Saito, y., Nakagawa, o., Kishimoto, i.e., Harada, m., Ogawa, e.g., Miyamoto, Y, Hamanaka, i.e., Kajiyama, n.a., Takahashi, n.a., Izumi, t.a., Kawakami, r.a., Tamura, n.a., Ogawa, y.a., Nakao, k.a., The effective of The selective ROCK inhibitor, Y27632, on-1-induced hyperthermia response in renal failure, e.g., balance, c.1999, and 5 g., balance: focus on Rho in crude disease.J.am.Soc.Nephrol.14, 2003, 261-264), cerebral vasospasm following subarachnoid hemorrhage (Shibuya, M., Suzuki, Y., Sugita, K., Saito, I., Sasaki, T., Takakura, K., Okamoto, S., Kikuchi, H., Takemae, T., Hidaka, H., Dose infection syndrome, AT877, implants 636 with an endothelial growth model group, ActaNeurochrome (Wien)107, 1990, 11-15; Shibuya, M., Suzuki, Y., Sugita, K., Saito, I., Sasaki, T., Takakura, K., Nagata, I., Kikuchi, H., Takemae, T., Hidaka, H., et al, Effect of AT877 one-way vacuum vasosp aft and electron absorption subarachnoid-robust retrieval of a pro-specific plate-controlled double-slab trial, J Neurosurg 76, 1992, 571-577; sato, M., Tani, E., Fujikawa, H., Kaibuchi, K., Involvement of Rho-kinase-mediated phosphorylation of myostatin chain in enhancement of nuclear vasospasm. circle Res 87, 2000, 195-200; miyagi, Y., Carpenter, R.C., Meguro, T., Parent, A.D., Zhang, J.H., alignment of rho A and rho kinase messenger RNAs in the basic array of a rat model of subarachnoid hemorrhage.JNeeurosurg 93, 2000, 471-; tachibana, e.g., Harada, t.t., Shibuya, m.saito, k.a., Takayasu, m.a., Suzuki, y.a., Yoshida, j.a., Intra-ocular infusion of facial hypertension (wien)141, 1999, 13-19), pulmonary hypertension (Sylvester, j.t., am.j.physical. lung.mol.physical.287, 2004, L624-L630) and ocular hypertension (Honjo, m.a., inaanii, m.a., Kido, n.a., mura, t. Yue, b.y.89119, Honda, y.1178, planta, t.a.1178, planta, HA, planta, et 1178; rao, P.V, Deng, P.F., Kumar, J.Epstein, D.L., Modulation of aqueous humor outflow facility by the enzyme rhokinase-specific inhibitor Y-27632.Invest Ophtalmol Vis Sci 42, 2001, 1029-. Other diseases associated with aberrant Rho/ROCK activity are Cancer (Aznar, S., Fernandez-Valeron, P., Espena, C., Lacal, J.C., RhoGTPases: potential candidates for anticancer therapy, Cancer Lett.206, 2004, 181-191; Yin, L. et al, Faudil inhibition, vascular inhibition factor-induced Cancer in vitro and in vivo, mol Cancer Ther5, 2007, 1517-25; Itoh, K., Yoshioka, K., Akedo, H., Yoshika, K., Akedo, H., S., E.C., S., E., Nat Med 5, 1999, 221-; genda, T.Sakamoto, M., Ichida, T.A., Asakura, H.A., Kojiro, M.A., Narumiya, S.A., Hirohashi, S.A., Cell mobility media associated with a kyro and Rho-associated protein kinase plant a crystalline enzyme in fibrous assays of human hepatocellular machinery 30, 1999, 1027-; somlyo, a.v., Bradshaw, d., Ramos, s., Murphy, c., Myers, c.e., Somlyo, a.p., Rho-kinase inhibitor recovery and in vivo diagnosis of human pro state cancercells biochem biophysis Res com 269, 2000, 652-; 1984, 837-843; chiba, Y., Misawa, M., Characteristics of musical chrysophanic purpuropeptor aids of antibiotic-induced aid hyperresponsive rates, Compsichem physical C Pharmacol Toxicol Endocrinol 111, 1995, 351-; chiba, Y., Takada, Y., Miyamoto, S., Mitsui Saito, M., Karaki, H., Misawa, M., Augmented acetyl choline-induced, Rho media Ca 2+Br J Pharmacol 127, 1999, 597-; chiba, Y., Sakai, H.Misawa, M., Australized chloretone-induced transformation of RhoA in branched smooth from anti-induced air high reactivity ratio, BrJ Pharmacol 133, 2001, 886-; iizuka, K., Shimizu, Y., Tsukagoshi, H., Yoshii, A., Harada, T.Dobashi, K., Murozono, T.A., Nakazawa, T.A., M.A., Evaluation of Y-27632, a rho-kinase inhibitor, as atronochloride in guineae' s.Eur J Pharmacol 406, 2000, 273-279), male erectile dysfunction (Andersson, K.E., Hedlund, P.A., New directive for erectile dysfunction)therapeutics, int.j.impot.res.14(suppl.1), 2002, S82-S92; chitaley, k., Wingard, c.j., Clinton Webb, r., Branam, h., Stopper, v.s., Lewis, r.w., Mills, t.m., Antagonism of Rho-kinase assays ratio selectivity nat Med 7, 2001, 119-; mills, t.m., Chitaley, k., Wingard, c.j., Lewis, r.w., Webb, r.c., Effect of Rho-kinase inhibition on vasoconstraction in the penile therapy.j Appl Physiol 91, 2001, 1269-: a target for training the early drawer of the system design. trends Pharmacol Sci.27, 2006, 492-7) and preterm labor (Niiro, N., Nishimura, J., Sakihara, C., Nakano, H., Kanaide, H., Up-registration of rho A and rho-kinase mRNAs in thermal rhythm severity prediction. biochem Biophys Res Commun 230, 1997, 356-359; tahara, M., Morisige, K., Sawada, K., Ikebuchi, Y., Kawagishi, R., Tasaka, K., Murata, Y., RhoA/Rho-kinase can be is inactivated in oxidized-induced ratio coupling, Endocrinology 143, 2002, 920-; kupittayanant, S., Burdyga, T., Wray, S., The effects of inhibiting Rho-associated kinase with Y-27632 on force and intracellular calcium in humonometer arch.443, 2001, 112-.
Inhibitors of rock have been suggested for the treatment of various diseases. They include cardiovascular diseases, such as hypertension (Satoh S., Kreutz R., Wilm C., Ganten D., PfitzerG., amplified agonist-induced Ca)2+-sensitization of coronary arterycontraction in genetically hypertensive rats.Evidence for altered signaltransduction in the coronary smooth muscle cells.J.Clin.Invest.94，1994，1397-1403；Mukai，Y.，Shimokawa，H.，Matoba，T.，Kandabashi，T.，Satoh，S.，Hiroki，J.，Kaibuchi，K.，Takeshita，A.，Involvementof Rho-kinase in hypertensive vascular disease：a novel theraFASEB J.15, 2001, 1062-1064; uehata, m., Ishizaki, t., Satoh, h., Ono, t., Kawahara, t., Morishita, t., Tamakawa, h., Yamagami, k., Inui, j., Maekawa, m., narumia, s., calcium sensing of smooth muscle media treated by a Rho-associated protein in hypertension. nature 389, 1997, 990-; and Masumoto, A., Hirooka, Y., Shimokawa, H., Hironaga, K., Setoguchi, S., Takeshita, A., Possible involvements of Rhokinase in The pulmonary of hypertension in humans. hypertension 38, 2001, 1307-; shimokawa, H., Cellular and molecular mechanisms of coronary artery spasm: jsson from animal models.jp Circ J64, 2000, 1-12; shimokawa, h., Morishige, k., Miyata, k., Kandabashi, t., Eto, y., Ikegaki, i., Asano, t., Kaibuchi, k., Takeshita, a., Longterm inhibition of rho-kinase a regression of aqueous nuclear delivery in adorpine model vivo, cardio Res 51, 2001, 169 one 177; utsunomiya, t., Satoh, s, Ikegaki, i., Toshima, y, Asano, t, Shimokawa, h, analytical effects of hydroxysurface, a Rho-kinase inhibitor, in an amino model of expression in br J pharmaceutical 134, 201, 1724-; sah, v.p., Hoshijima, m., Chien, k.r., Brown, j.h., Rho is required for Galphaq and alpha 1-acquired receptor signal-637in cardio cells, diagnosis of Ras and Rho pathways.j biol chem 271, 1996, 31185 1190; kuwahara, K., Saito, Y., Nakagawa, O., Kishimoto, I., Harada, M., Ogawa, E., Miyamoto, Y., Hamamaka, I., Kajiyama, N., Takahashi, N., Izumi, T., Kawakami, R., Tamura, N., Ogawa, Y., Nakao, K., The efficiencies of The selective ROCK inhibitor, Y27632, on-1-induced hyperthermophilic stress in renal failure, reliable invasion of Rho/K pathway in cardiac tissue cells, FETTY 452, renal failure, Sharponic stress, 314, Sharpnage, C.318: focus on Rho in secondary disease.J.Am.Soc.Nephrol.14, 2003, 261-264), cerebral vasospasm after subarachnoid hemorrhage (Shibuya, M., Suzuki, Y., Sugita, K., Saito, I., Sasaki, T., Takakura, K., Okamoto, S., Kikuchi, H., Takemae, T., Hidaka, H., Dose evaluation Trim of a novel calcium antagonist, AT877, in Patients 636 and tissue sample subarachnoid repair (Actaneuro Wien)107, to 11-15, shine, M., Y., K., Sagita, Sakii, Sasang, Saik, S., Saik, K., Saybolt, H., repair, K., 7, repair, K., repair, K., repair, et al, repair, 2000, 195-; miyagi, Y., Carpenter, R.C., Meguro, T., Parent, A.D., Zhang, J.H., alignment of rho A and rho kinase messenger RNAs in the basic array of a rat model of subarachnoid hemorrhage.J.Neurosuring 93, 2000, 471-; tachibana, e.g., Harada, t., Shibuya, m.saito, k.a., Takayasu, m.a., Suzuki, y.a., Yoshida, j., Intra-annular infusion of failure hydrochloride for treating vasospasm followings subachhii a 9, 13-19), pulmonary hypertension (Sylvester, j.t., am.j.physiol.lung cell.mol.physiol.287, 2004, L624-L630) and ocular hypertension (Honjo, m., Inatani, m., Kido, n., Sawamura, t., Yue, b.y., Honda, y., Tanihara, h., Effects of proteinkinase inhibitor, HA1077, on intraepithelial pressure and outer surface sensitivity in the ear opthalmol 119, 1171-2001 1178; rao, P.V, Deng, P.F., Kumar, J.Epstein, D.L., Modulation of aqueous humor aqueous surface by the Rho kinase-specific inhibitor Y-27632.Invest OphthalmolVis Sci 42, 2001, 1029-. Furthermore, due to their muscle relaxation properties, they are also suitable for asthma (Roberts, J.A., Raeburn, D.D., Rodger, I.W., Thomson, N.C., company of in vivo air responsive and in vitro microbial sensing to methyl alcohol in man.Thorax 39; 1984, 837. 843; Chiba, Y., Misawa, M.A., chromatography of organic chlorine polymers in aqueous solutions of organic-induced air responsive and C.compressive polymers in aqueous emulsion 111, 1995, 351, Y.A., Takada, Y.A., Miyamo, Miyawa, Miyasuc.C. biochemical analysis, Miyawed.C.A., Miyawed.C.C. alcoholic copolymer 111, 1995, 351, Ca, Y.A., Miyawed.A., Miyawed.S., Miyawed.A., Miyawed.A.A., Miyawed.A.A.C. biological absorbent, Miyawed.A.A. 2+(ii) a sensorionf branched mucosal reaction in an anti-induced airborne process. Br J Pharmacol 127, 1999, 597-600; chiba, Y., Sakai, H.Misawa, M., Augmented acetyl choline-induced translocation of RhoA in branched polysaccharide from induced air waterborne reactivity. BrJ Pharmacol 133, 2001, 886-; izuka, K., Shimizu, Y., Tsukagoshi, H., Yoshii, A., Harada, T.Dobashi, K., Murozono, T, Nakazawa, T.A., Mori, M., Evaluation of Y-27632, arm-kinase inhibitor, as a branched in gulinea pixels Eur J Pharmacol406, 2000, 273-279), male erectile dysfunction (Andersson, K.E., Hedlund, P.W. directions for male erectile dysfunction therapeutics J.Res.14 (Suppl.1), 2002, S82-S92; chitaley, K.Wingard, C.J., Clinton Webb, R., Branam, H., Stopper, V.S., Lewis, R.W., Mills, T.M., Antagonism of Rho-kinase stimulation rate conversion maintenance, via a nitrile oxide depletion potential. Nat Med 7, 2001, 119-; mills, t.m., Chitaley, k., Wingard, c.j., Lewis, r.w., Webb, r.c., Effect of Rho-kinase inhibition on the urinary circulation, j Appl Physiol 91, 2001, 1269-: a target for cutting urea blader dysfunction. trends pharmacol sci.27, 2006, 492-7) and preterm labor (Niiro, N., Nishimura, J., Sakihara, C., Nakano, H., Kanaide, H., Up-alignment of rho A andro-kinase mRNAs in the rate mycometric degradation prediction. Tahara, M., Morisige, K., Sawada, K., Ikebuchi, Y., Kawagishi, R., Tasaka, K., Murata, Y., RhoA/Rho-kinase can be is inactivated in oxidized-induced ratio coupling, Endocrinology 143, 2002, 920-; kupittayanant, S., Burdyga, T., Wray, S., The effects of inhibiting Rho-associated kinase with Y-27632 on force and intracellular calcium in human microorganisms Arch.443, 2001, 112-. Several recent studies have reported the beneficial effects of ROCK inhibitors on ischemia-reperfusion and myocardial infarction. In these studies, ROCK inhibitor Y-27632 and fasudil reduced ischemia-reperfusion injury, myocardial infarction area and myocardial fibrosis in response to experimental Myocardial Infarction (MI) and in a rat model of chronic hypertension caused by congestive heart failure (see above (fuse, V., Badimon, L., Badimon, JJ, Chesebro, JH, The pathogenesis of cardiovascular disease and The interventional cardiovascular syndrome (2), N Engl J Med 326, 1992, 310 and 318; Shimokawa, H., Cellular and molecular mechanics of cardiovascular disease spasm: lasson and models, Jpn Circ J64, 2000, 1-12; Shimokawa, Migris H., Migris, Mitsu, Kande, et al, in response to experimental Myocardial Infarction (MI), and congestive heart failure, and chronic hypertension. Eto, Y, Ikegaki, I, Asano, T, Kaibuchi, K, Takeshita, A, Long termination of Rho-kinase indexes a regression of iterative coronaries in a stress model in vivo, Cardiovasc Res 51, 2001, 169, 177; utsunomiya, t., Satoh, s., Ikegaki, i., Toshima, y, Asano, t, Shimokawa, h., artificial effects of hydroxysurface, a Rho-kineticiuth, in a Canine model of effect origin, br J Pharmacol 134, 201, 1724-; shimokawa, H., Iinuma, H., Kishida, H., et al, antibiotic effect of failure, aRaho-kinase inhibitor, in patents with stable effect in the same: a multicentrsttutdy (abstrat). Circulation 104[ Suppl II]，2001，II691；Morishige K，Shimokawa H，Eto Y，Kandabashi T，Miyata K，Matsumoto Y，HoshijimaM，Kaibuchi K，Takeshita A，Adenovirus-mediated transfer ofdominant-negative rho-kinase induces a regression of coronaryarteriosclerosis in pigs in vivo.Arterioscler Thromb Vasc Biol 21，2001，548-554；Kandabashi T，Shimokawa H，Mukai Y，Matoba T，KunihiroI，Morikawa K，Ito M，Takahashi S，Kaibuchi K，Takeshita A，Involvement of rho-kinase in agonists-induced contractions ofarteriosclerotic human arteries.Arterioscler Thromb Vasc Biol 22，2002，243-248；Liu MW，Roubin GS，King SB 3rd，Restenosis after coronaryangioplasty.Potential biologic determinants and role of intimalhyperplasia.Circulation 79，1989，1374-1387；Shibata R，Kai H，SekiY，Kato S，Morimatsu M，Kaibuchi K，Imaizumi T，Role ofRho-associated kinase in neointima formation after vascular injury.Circulation 103，2001，284-289)。
In addition, ROCKs can interact with other signaling pathways that lead to inhibition of the activation of phosphoinositide-3 kinase (PI-3K), the endothelial nitric oxide synthase (eNOS) pathway, and the plasminogen activator inhibitor-1 (PAI-1), which can promote endothelial dysfunction, such as restenosis and atherosclerosis. Thus, ROCK inhibitors have been suggested for the treatment of restenosis and atherosclerosis (see above (Morisige K, Shimokawa H, Eto Y, Kandaabashi T, MiyataK, Matsumoto Y, Hoshijima M, Kaibuchi K, Takeshita A, Adenovir-mediated transfer of negative-negative rho-kinase assays of synthesis of synergistic aryl in peptides in viruses. Arioscopist Thromb Bio 21, GS 2001, 548 554; Kandachi T, Shimokawa H, Mukai Y, Matoba T, Kunihii I, Morikawa K, Ito M, Takahashi S, Kaibushi K, Takeshishi A, Takashishi A, Thrombia of yeast, Va IV of molecular of nucleic acids in viruses 22, Ashishi, MW of lipase IV, Vab IV, S, Takauchia K, Takayakashova K, Takashiwa A, Shikayak-kinase in, Shikajima M, Vashijima M, Vashikunishikushikushikushikushiwa I, Va I S, Va III, Va I S, S rd(iii) respiratory coronary anatomical definitions and role of intrabiological science circulation 79, 1989, 1374) 1387; shibata R, Kai H, Seki Y, Kato S, Morimasu M, Kaibuchi K, Imaizumi T, Role of Rho-associated kinase in neo formation after vacuum infusion. circulation 103, 2001, 284 289) and Iwasaki, H. et al, High glucose induced kinase inhibitor-1 expression of throughRho/Rho-kinase-mediated NF-kappaB activity in bone antigen connected cells.
Intimal thickening of vessels following vein graft surgery is a major cause of late graft failure. In the study of the ROCK inhibitor fasudil, intimal thickening and Vascular Smooth Muscle Cell (VSMC) proliferation were significantly inhibited, and VSMC apoptosis increased in several weeks after this procedure, suggesting that ROCK inhibitors may be useful as therapeutic agents for graft protection (Morishige K, Shimokawa H, Eto Y, Kandabashi T, Miyata K, Matsumoto Y)，Hoshijima M，Kaibuchi K，Takeshita A，Adenovirus-mediated transfer of dominant-negative rho-kinase induces aregression of coronary arteriosclerosis in pigs in vivo.ArteriosclerThromb Vasc Biol 21，2001，548-554；Kandabashi T，ShimokawaH，Mukai Y，Matoba T，Kunihiro I，Morikawa K，Ito M，TakahashiS，Kaibuchi K，Takeshita A，Involvement of rho-kinase inagonists-induced contractions of arteriosclerotic human arteries.Arterioscler Thromb Vasc Biol 22，2002，243-248；Liu MW，RoubinGS，King SB 3rd，Restenosis after coronary angioplasty.Potentialbiologic determinants and role of intimal hyperplasia.Circulation 79，1989，1374-1387；Shibata R，Kai H，Seki Y，Kato S，MorimatsuM，Kaibuchi K，Imaizumi T，Role of Rho-associated kinase inneointima formation after vascular injury.Circulation 103，2001，284-289)。
Injury to the brain and spinal cord of adult vertebrates activates ROCKs, thereby causing neurodegeneration and inhibiting nerve regeneration, for example, axon growth and sprouting (bioto, h., Furuyashiki, t., Ishihara, h., Shibasaki, y., Ohashi, k., Mizuno, k., Maekawa, m., ishizki, t., Narumiya, s., a clinical role for a Rho-assailatedkinase, p160ROCK, in determining axon output growth in mammalia cnsneurons. neuron 26, 2000, 431-. After acute neuronal injury in mammals (spinal cord injury, traumatic brain injury), ROCK is inhibited, new axon growth is induced, axons re-cross lesions within the CNS (healing injuries), regeneration is promoted and functional recovery is enhanced (see above (pets, s.l. et al, Rho kinase: a targeting for healing nerve fibers sci.27, 2006, 492-7) and Hara, m. et al, Protein kinase by bone repair surgery injection into nerve fibers surgery J.nerve fibers 93, 94-101; fountain, A.E. patent, tissue B.T, tissue repair, bone repair, nuclear repair, Protein injection, Protein cement repair, ROCK repair, cement, ROCK repair, cement, 2004, 155-164). Thus, ROCK inhibitors are also useful in regenerative (rehabilitation) treatment of CNS disorders, such as spinal cord injury, acute neuronal injury (stroke, traumatic brain injury) (Okamura N et al, compressor efficiencies of failure, a Rho-kinase inhibitor, on-specific imaging in stress-nerve theory. J ocular pharmaceutical theory. 23, 2007, 207-12; Yagita Y et al, Rho-enzyme activation in endothelial cells suspensions to expansion of failure after focal isolation. JNeeurosis Res.85, 2007, 2460-9), Parkinson's disease, Alzheimer's disease (modified of nerve disease, attention, nerve disease, 2. AIDS, 2. and 3. 9), and also in neurological disorders of depression, AIDS, 2. D. and S. 3. D. Pat. No. 3. and S. D. Pat. 3. and S. 3. and S. 3. D. Pat. No. 3. and S. 3. D. nerve degeneration of nerve disease. Other neurodegenerative disorders in which ROCK inhibitors are expected to be useful are Huntington's disease (Shao J, Welch WJ, Diprospero NA, Diamond MI. phosphorylation of profile by ROCK1 regulation of polyglutaminageformation. mol Cell biol.2008 Sep. (28 (17): 5196-208; Shao J, Welch WJ, Diamond MI. ROCK and PRK-2 medium the inhibitory effect of Y-27632 on polyglutaminageformation. FEBS Ley 28; 582 (12): 1637-42), spinal muscular atrophy (Bowman M, Shafefefefefe D, Kothray R.Smn deletion salts II precursors to Rhogreen A/32. lateral sclerosis and hardening of ROCK. 32. 9. and 32. lateral sclerosis. In neurodegeneration (e.g., stroke) (Okamura N et al, pigment effects of facial pain, a Rho-kinase inhibitor, on specific organs in peptide-protein emulsions of facial pain. J. ocular pharmacological theory. 23, 2007, 207-12; Yagita Y et al, Rho-kinase inhibition in endothelial cells to expansion of topical brain sclerosis. 85, 2007, 2460-9) and inflammatory and demyelinating diseases (e.g., multiple sclerosis) (Sun X et al, The specific hormone receptor therapeutic tissue of facial pain. 10. hormone, biological tissue of bone marrow tissue of bone tissue of bone marrow tissue of bone marrow tissue of bone marrow tissue of bone marrow tissue of bone tissue of bone, 10796-; inhibition of the Rho/ROCK pathway has also been shown to be effective in other animal models of Tatsumi, S. et al, invasion of Rho-kinase in immobilized and neuropathic paintgrouphsphorylation of glycosylated alkane-rich C-kinase (MARCKS) 131, 2005, 491-498).
ROCK inhibitors have been shown to have anti-inflammatory properties by reducing the release of cytokines (e.g., TNF α). Thus, they may be used in the treatment of neuroinflammatory disorders such as stroke, multiple sclerosis, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis and inflammatory pain, as well as other inflammatory disorders such as rheumatoid arthritis, osteoarthritis, osteoporosis, asthma, irritable bowel syndrome or inflammatory bowel disease. (Segain J.P., Rho kinase block precursors in video nuclear factor kappa restriction: evidence in Crohn's disease and experimental science.124 (5), 2003, 1180-7). Furthermore, recent reports indicate that inhibition of ROCK can disrupt chemotaxis of inflammatory cells and inhibit smooth muscle contraction in models of pulmonary inflammation associated with asthma. Thus, inhibitors of The Rho/ROCK pathway should be useful in The treatment of asthma (see above (Sun X et al, The selective Rho-kinase inhibitor fast is technical and therapeutic in experimental autoimmune genetic polymorphism. J.Neuromimetic. 180, 2006, 126-34) and Kawaguchi A, Ohmori M, Harada K, Tsuoroka S, Sugimoto K, Fujimura A. The effective Rho enzyme inhibitor Y-27632 on therapeutic promoter, aggregate and fusion in human aggregate nucleic acids, Eur J.403, 2000, 203, Lorsz, Bilaleurooid. J.160, Rho J.M.2001. coli J.5749, Rho J.M.A.579, Rho J.M.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A.A. 1alpha-induced catalysis activity and microtubular organization and chemotaxis. jimmunol 168, 2002, 400-410; thoracius K et al, Protective effect of facial, a Rho-kinase inhibitor, on-chemokine expression, leukakyterrestiment, and heterocyclic apoptosis in therapeutic efficacy in therapy J Leukoc biol.79, 2006, 923-31).
Since ROCK inhibitors reduce Cell proliferation and Cell migration, they may be used for the treatment of cancer and tumor metastasis (Aznar, S., Fernandez-Valeron, P., Espena, C., Lacal, J.C., Rho GTPases: potential candidates for anticancer therapy. cancer Lett.206, 2004, 181-191; Yin, L. et al, Fassian bits variable and soluble growth factor in vitro and in vivo. MolCancer Ther 5, 2007, 1517-25.Itoh, K., Yoshioka, K., Akedo, H.uhahahahahaase, M.Ishiki, T.T., nuclear, S.Anmiak, Saitian. sample, Cell suspension, Cell 1999, Cell, human tissue, Cell, animal tissue, Cell, A.V., Bradshaw, D., Ramos, S., Murphy, C., Myers, C.E., Somlyo, A.P., Rho-kinase inhibitor recovery simulation and video isolation of human promoter cells biochem Biophys Commun 269, 2000, 652-. ROCK inhibitors may also be beneficial in diseases with impaired blood brain barrier function such as HIV-1 encephalitis (Persidski Y et al, Rho-mediated regulation of light junctions due to monoclonal hybridization access the blood-brain barrier-barrier in HIV-1 enphalitis (HIVE), blood.107, 2006, 4770-4780) and Alzheimer 'S disease (Man S-M et al, Peripheral T cell above MIP-1a enhancement peptide amplification in Alzheimer' S disease. Neurobiological of Aging 28, 2007, 485-496).
Furthermore, there is evidence that ROCK inhibitors inhibit Cytoskeletal rearrangement caused by viral invasion, and thus they also have potential therapeutic value in antiviral and antibacterial applications (Favoreel HW, cytological rearrancing and cell extensions for the US3 kinase of an alphaherpesvirus arm associated with enhanced expression with the Sci US S102 (25), 2006, 8990-5).
It has been reported that ROCKs interfere with insulin signaling through serine phosphorylation of insulin receptor substrate-1 (IRS-1) in cultured VSMC. In skeletal muscle and aortic tissue of Zucker obese rats, activation of RhoA/ROCK was observed. Fasudil inhibits ROCK for four weeks, resulting in a reduction in blood pressure, correction of glucose and lipid metabolism, and improvement of insulin signaling and endothelial dysfunction. In another experiment, fasudil given to OLETF rats at high doses completely inhibited the development of diabetes, obesity and dyslipidemia and increased serum adiponectin levels. Thus, ROCK inhibitors may be useful in The treatment of insulin resistance and diabetes (Nakamura Y et al, Marked in diabetes of insulin genetic description by suppression of The Rho/Rho-kinase pathway biochem Res Commun.350(1), 2006, 68-73; Kikuchi Y et al, ARho-kinase inhibitor, facial, depression of diabetes and diabetes of insulin-metabolic pathway insulin in insulin-metabolic pathway J Endocrinol.192(3), 2007, 595-603; Goyo A et al, The Rho-kinase inhibitor, facial, inflammatory polysaccharides in diabetes of diabetes and diabetes of diabetes mellitus J.2007, 11-242, 242. 1.2007).
Fasudil, a ROCK inhibitor, increases cerebral blood flow and has neuroprotective effects in CNS ischemic conditions. ROCK inhibitors are expected to be useful in the treatment of ischemic CNS disorders and thus may improve the functional outcome in patients with stroke, vascular or AD type dementia (Okamura N et al, vasodialator effects of facial, a Rho-kinase inhibitor, on-specific enzymes in stroke-protein plasma chemotherapeutics. jocul pharmaceutical. 23, 2007, 207-12; Yagita Y et al, Rho-kinase in endovenous cells to expansion of the functional physiological metabolism. j Neurosci res.85, 2007, 2460-9).
Because of the effects of Y-27632 and fasudil in animal models of epileptogenesis, ROCK inhibitors have been suggested for the treatment of epilepsy and seizure disorders (Inan SY, Bu yu kafsark. Antiepitic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice, Br. J. Pharmacol. advance on line publication, 9 June 2008; doi: 10.1038/bjp.2008.225)
ROCK inhibitors are also expected to be useful in the treatment of glaucoma (Honjo, M., Inatani, M., Kido, N., Sawamura, T., Yue, B.Y., Honda, Y., Tanihara, H., Effect protein kinase inhibitor, HA1077, on-intercalar pressure and outflow failure in ribbon, Arch Ophthalmol 119, 2001, 1171-type 1178, Rao, P.V, Deng, P.F., Kumar, J.Epstein, D.L., Modulation of aqueous humor failure by the Rho kinase-specific inhibitor Y-27632. Invhthalol Vis 42, 1029, 1037, psoriasis and benign prostatic hyperplasia.
Furthermore, there is evidence that ROCK inhibitors inhibit cytoskeletal rearrangement caused by viral entry, and thus they also have potential therapeutic value in antiviral and antibacterial applications.
Since ROCKs are generally involved in morphogenesis, connectivity and plasticity of neurons, they are expected to be useful in the treatment of psychiatric disorders such as depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders.
ROCK inhibitors are described, for example, in WO 2007/026920, WO 2005/074643 and WO 2004/016597. However, their affinity and selectivity or their pharmacological properties are not yet very satisfactory.
Reaction schemes and experiments
The following abbreviations have the indicated meanings. ADDP means 1, 1' - (azodicarbonyl) bipiperidine; AD-mix-beta means (DHQD)2PHAL、K3Fe(CN)6、K2CO3And K2SO4A mixture of (a); 9-BBN means 9-borabicyclo (3.3.1) nonane; boc is t-butyloxycarbonyl; (DHQD)2PHAL refers to hydrogenated quinidine 1, 4-phthalazinediyl diethyl ether; DBU means 1, 8-diazabicyclo [5.4.0]Undec-7-ene; DIBAL refers to diisobutylaluminum hydride; DIEA refers to diisopropylethylamine; DMAP refers to N, N-dimethylaminopyridine; DMF means N, N-dimethylformamide; dmpe refers to 1, 2-bis (dimethylphosphino) ethane; DMSO refers to dimethylsulfoxide; dppb refers to 1, 4-bis (diphenylphosphino) -butane; dppe refers to 1, 2-bis (diphenylphosphino) ethane; dppf refers to 1, 1' -bis (diphenylphosphino) ferrocene; dppm refers to 1, 1-bis (diphenylphosphino) methane; EDAC & HCl refers to 1- (3-dimethylaminopropyl) -3-ethylcarbodiimide hydrochloride; fmoc refers to fluorenylmethoxycarbonyl; HATU refers to O- (7-azabenzotriazol-1-yl) -N, N' -tetramethyluronium hexafluorophosphate; HMPA means Hexamethylphosphoramide; IPA means isopropanol; MP-BH3Is macroporous methyl polystyrene cyano triethylamine borohydride; TEA refers to triethylamine; TFA means trifluoroacetic acid; tetrahydrofuran refers to tetrahydrofuran; NCS refers to N-chlorosuccinimide; NMM refers to N-methylmorpholine; NMP refers to N-methylpyrrolidine; PPh3Refers to triphenylphosphine.
In order to provide an illustration of the method and conceptual aspects of the invention that are believed to be the most useful and readily understood, the following reaction schemes are provided. The compounds of the invention may be prepared by synthetic chemical methods, examples of which are given herein. It will be understood that the order of steps in the method may be varied, that reagents, solvents and reaction conditions may be substituted for those specifically recited, and that susceptible moieties may be protected and deprotected as desired.
Reaction scheme
As shown in scheme 1, compounds of formula (1), wherein X1、X2And X3As described herein, can be reacted with methyl 4-isocyanatobenzoate to provide compounds of formula (2). The reaction is generally carried out in a solvent such as, but not limited to: tetrahydrofuran. Methyl 4-isocyanatobenzoate is generally added at low temperature and then stirred at room temperature. The compound of formula (3) can be prepared by reacting the compound of formula (2) with an aqueous lithium hydroxide solution. The reaction is generally carried out in a solvent such as, but not limited to: tetrahydrofuran, methanol or mixtures thereof. Using coupling conditions known to those skilled in the art and readily available in the literature, compounds of formula (3) can be reacted with amines of formula (3A), wherein R is 5Is hydrogen or as described herein, provides compounds of formula (4), which are representative of the compounds of the present invention.
As shown in scheme 2, compounds of formula (1), wherein X1、X2And X3As described herein, can be reacted with p-nitrophenylisocyanate to provide a compound of formula (5). The reaction is generally carried out in a solvent such as, but not limited to: tetrahydrofuran. The compound of formula (5) may be treated with a hydrogen balloon in the presence of 10% Pd on carbon to provide the compound of formula (6). The reaction is generally carried out at ambient temperature in a solvent such as, but not limited to: dimethylformamide (DMF). Using coupling conditions known to those skilled in the art and readily available in the literature, compounds of formula (6) can be reacted with acids of formula (6A), wherein R is5As described herein, compounds of formula (7) are provided which are representative of the compounds of the present invention.
Reaction scheme 3
As shown in scheme 3, compounds of formula (1) wherein X1、X2And X3As described herein, 4-bromophenyl isocyanate may be reacted with to provide compounds of formula (8). The reaction is generally carried out in a solvent such as, but not limited to: tetrahydrofuran. Using Suzuki coupling conditions known to those skilled in the art and readily available in the literature, a compound of formula (8) can be reacted with a boronic acid (or suitable boronic ester) of formula (9A), wherein R is 5As described herein, compounds of formula (9) are provided which are representative of the compounds of the present invention.
As shown in scheme 4, those skilled in the artCompounds of formula (8) wherein X is1、X2And X3As described herein, can be reacted with tert-butyl 4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylate to provide compounds of formula (10). The compound of formula (11) can be prepared by treating the compound of formula (10) with an acid such as, but not limited to, trifluoroacetic acid. The reaction is generally carried out at room temperature in a solvent such as, but not limited to: dichloromethane. A compound of formula (11) may be reacted with a compound of formula (12A) in the presence of a carboxyl activating agent (such as, but not limited to, N- (3-dimethylaminopropyl) -N' -ethylcarbodiimide hydrochloride) and a coupling agent (such as, but not limited to, 1-hydroxybenzotriazole hydrate), wherein R is13As described herein, compounds of formula (12) are provided. The reaction is generally carried out at room temperature in a solvent such as, but not limited to: n, N-dimethylformamide.
Alternatively, the compound of formula (12) may be treated with hydrogen in the presence of palladium on carbon to provide the compound of formula (13). The reaction is generally carried out under pressure in a solvent such as, but not limited to: tetrahydrofuran or N, N-dimethylformamide. A compound of formula (13) may be reacted with a compound of formula (12A) in the presence of a carboxyl activating agent (such as, but not limited to, N- (3-dimethylaminopropyl) -N' -ethylcarbodiimide hydrochloride) and a coupling agent (such as, but not limited to, 1-hydroxybenzotriazole hydrate), wherein R is 13As described herein, compounds of formula (14) are provided. The reaction is generally carried out at room temperature in a solvent such as, but not limited to: n, N-dimethylformamide.
Aqueous potassium hydroxide and a phase transfer catalyst (such as, but not limited to, tetrabutylammonium bromide) may be added to 4-hydroxy-1-piperidine-1-carboxylic acid tert-butyl ester and 1-fluoro-4-nitrobenzene to provide 4- (4-nitrophenoxy) piperidine-1-carboxylic acid tert-butyl ester. Tert-butyl 4- (4-aminophenoxy) piperidine-1-carboxylate may be prepared by the reaction of tert-butyl 4- (4-nitrophenoxy) piperidine-1-carboxylate with hydrogen in the presence of palladium on carbon. The reaction is generally carried out under pressure in a solvent such as, but not limited to: tetrahydrofuran or N, N-dimethylformamide. Tert-butyl 4- (4-aminophenoxy) piperidine-1-carboxylate may be reacted with bis (2, 5-dioxopyrrolidin-1-yl) carbonate and pyridine (in acetonitrile) followed by addition of a base (such as, but not limited to, diisopropylethylamine) and a compound of formula (15A) to provide a compound of formula (15). The reaction is generally carried out at room temperature. The compound of formula (16) may be prepared by treating the compound of formula (15) with an acid such as, but not limited to, trifluoroacetic acid. The reaction is generally carried out at room temperature in a solvent such as, but not limited to: dichloromethane. A compound of formula (16) may be reacted with a compound of formula (12A) in the presence of a carboxyl activating agent (such as, but not limited to, N- (3-dimethylaminopropyl) -N' -ethylcarbodiimide hydrochloride) and a coupling agent (such as, but not limited to, 1-hydroxybenzotriazole hydrate), wherein R is 13As described herein, compounds of formula (17) are provided. The reaction is generally carried out at room temperature in a solvent such as, but not limited to: n, N-dimethylformamide.
In order to provide an illustration of the method and conceptual aspects of the invention that are believed to be most useful and readily understood, the following examples are provided. ACD/ChemSketch Version 12.01(2009, 13.5.9) (Advanced Chemistry Development Inc., Toronto, Ontario) or ChemDraw was usedExemplary compounds are named by ver.9.0.5(Cambridge soft, Cambridge, MA). Using ChemDrawVer.9.0.5(Cambridge Soft, Cambridge, MA) names the intermediates.
Experiment of
Example 1
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 1A
4- (isoindoline-2-carboxamido) benzoic acid methyl ester
Isoindoline (1.693mL, 14.47mmol) was dissolved in tetrahydrofuran (20mL) and cooled to 0 ℃; methyl 4-isocyanatobenzoate (2.18g, 12.06mmol) was added via syringe and the resulting mixture was heated to ambient temperature and then stirred overnight. The solution was concentrated to give a slurry, diluted with ether and filtered to provide the title compound.
Example 1B
4- (isoindoline-2-carboxamido) benzoic acid
Methyl 4- (isoindoline-2-carboxamido) benzoate (1.65g, 5.57mmol) was dissolved in tetrahydrofuran (30mL) and methanol (15.00mL), followed by lithium hydroxide (11.14mL, 22.27mmol), and the mixture was stirred at ambient temperature over the weekend. The organic solvent was removed in vacuo, the aqueous layer was adjusted to pH-3 with 2N aqueous HCl, and the resulting solid was filtered, washed with water, and dried to provide the title compound.
Example 1C
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
4- (isoindoline-2-carboxamido) benzoic acid (150mg, 0.531mmol) and 1-hydroxybenzotriazole hydrate (122mg, 0.797mmol) were dissolved in dimethylformamide (3ml), followed by the addition of 3-phenylpropan-1-amine (110mg, 0.797mmol) and N- (3-dimethylaminopropyl) -N' -ethylcarbodiimide hydrochloride (153mg, 0.797 mmol). The homogeneous solution was stirred at ambient temperature overnight. Diluting the solution with water to obtain a precipitate, filtering, washing with cooled ethyl acetate, washing with ether, and vacuum dryingThe title compound is provided.1HNMR(400MHz，DMSO-d6δ ppm at 90 ℃ (bs, 1H), 7.93-7.98(m, 1H), 7.73-7.76(m, 2H), 7.61-7.64(m, 2H), 7.32-7.36(m, 2H), 7.27-7.32(m, 2H), 7.24-7.28(m, 2H), 7.19-7.24(m, 2H), 7.13-7.18(m, 1H), 4.79(s, 4H), 3.30(q, J ═ 6.5Hz, 2H), 2.65(t, J ═ 7.6Hz, 2H), 1.86(p, J ═ 7.3Hz, 2H); MS (ESI (+)) M/e 400(M + H) +.
Example 2
N- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 2A
4- (5-Fluoroisoindoline-2-carboxamido) benzoic acid methyl ester
The title compound was prepared as described in example 1A, using 5-fluoroisoindoline instead of isoindoline
Example 2B
4- (5-fluoroisoindoline-2-carboxamido) benzoic acid
The title compound was prepared as described in example 1B, using methyl 4- (5-fluoroisoindoline-2-carboxamido) benzoate instead of methyl 4- (isoindoline-2-carboxamido) benzoate.
Example 2C
4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 1C, using 4- (5-fluoroisoindoline-2-carboxamido) benzoic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid, and tert-butyl 4- (aminomethyl) benzylcarbamate instead of 3-phenylpropan-1-amine.
Example 2D
N- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate (392mg, 0.756mmol) was dissolved in dichloromethane, treated with trifluoroacetic acid (582. mu.l, 7.56mmol), stirred at ambient temperature for 3 hours and then concentrated to dryness. The resulting solid was triturated with ether, collected and dried in vacuo to provide the title compound. 1HNMR(400MHz，DMSO-d6)δppm 4.01(q，J＝5.6Hz，2H)，4.46(d，J＝6.0Hz，2H)，4.76(d，J＝7.9Hz，4H)，7.08-7.29(m，2H)，7.32-7.44(m，5H)，7.67(d，J＝8.7Hz，2H)，7.76-7.86(m，2H)，8.12(s，2H)，8.63(s，1H)，8.91(t，J＝6.2Hz，1H)；MS(ESI(+))m/e 419(M+H)+。
Table 3.
The following examples were prepared essentially as described in example 1, substituting suitably substituted isoindoline for isoindoline in example 1A and substituting a suitable amine for 3-phenylpropan-1-amine in example 1C. Some products were purified by flash chromatography while others were purified by reverse phase HPLC; some compounds also require Boc-deprotection after amide coupling as described in example 2D. Accordingly, some of the examples were isolated as trifluoroacetate salts.
Example 132
N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide
A solution of 5-cyano-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide (30mg, 0.9mmol) in sulfuric acid (0.1mL) and trifluoroacetic acid (0.3mL) was stirred at room temperature for 16 h. The reaction was treated with ice and the suspension was stirred for 10 minutes and filtered. Washing the collected solid with water and vacuum drying; the solid was purified by reverse phase HPLC to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 8.61(s，1H)，8.26(t，J＝5.7Hz，1H)，7.97-8.00(bs，1H)，7.81-7.86(m，2H)，7.75-7.79(m，2H)，7.63-7.68(m，2H)，7.44(d，J＝7.8Hz，1H)，7.34-7.39(bs，1H)，4.81-4.82(bs，4H)，3.16-3.24(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 367(M+H)+。
Example 272
2- { [4- (Propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester
Example 272A
4-amino-N-propylbenzamides
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
A solution of 4-nitro-N-propylbenzamide (800mg, 0.1mmol) in 40ml tetrahydrofuran was treated with 30psi of hydrogen at room temperature in a pressure bottle in the presence of 160mg of 20% Pd/carbon for 30 minutes. The suspension was filtered through a nylon membrane and concentrated to provide the title compound.
Example 272B
2- { [4- (Propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester
A solution of 4-amino-N-propylbenzamide (390mg, 2.19mmol), bis (2, 5-dioxopyrrolidin-1-yl) carbonate (700mg, 2.74mmol) and pyridine (0.18mL, 2.19mmol) in acetonitrile (5mL) was stirred at ambient temperature for 30 min. Diisopropylethylamine (0.85mL, 6.6mmol) was added, followed by dropwise addition of a suspension of isoindoline-5-carboxylic acid methyl ester hydrochloride (538mg, 2.52mmol) and diisopropylethylamine (0.46mL, 4.4mmol) in 1-methyl-2-pyrrolidone (8mL) via syringe over 5 minutes. The reaction became a suspension and was stirred for 3 hours. The reaction was treated with water (30mL) and the resulting suspension was stirred for 5 minutes and filtered. The collected solid was washed with water and dried in vacuo to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 8.63(s，1H)，8.26(t，J＝5.6Hz，1H)，7.94-7.97(m，1H)，7.90-7.96(m，1H)，7.75-7.78(m，2H)，7.63-7.67(m，2H)，7.52(d，J＝7.9Hz，1H)，4.83-4.86(m，4H)，3.87(s，3H)，3.16-3.22(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e382(M+H)+。
Example 273
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid
The title compound was prepared as described in example 1B, using 2- { [4- (propyl)Carbamoyl) phenyl]Carbamoyl } isoindoline-5-carboxylic acid methyl ester instead of 4- (isoindoline-2-carboxamido) benzoic acid methyl ester.1H NMR(300MHz，DMSO-d6)δppm12.90-13.07(bs，1H)，8.62(s，1H)，8.26(t，J＝5.7Hz，1H)，7.88-7.93(m，2H)，7.75-7.78(m，2H)，7.63-7.67(m，2H)，7.49(d，J＝7.9Hz，1H)，4.83-4.85(bs，4H)，3.16-3.24(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；(ESI(+))m/e 368(M+H)+.
Example 274
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
5-Nitro-N- [4- (propylcarbamoyl) phenyl at room temperature in the presence of 11mg of 10% Pd/carbon]A solution of-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide (37mg, 0.1mmol) in 1mL dimethylformamide was treated with a balloon of hydrogen overnight. The suspension was filtered through celite and purified by reverse phase HPLC to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 8.51(s，1H)，8.24(t，J＝5.6Hz，1H)，7.74-7.78(m，2H)，7.62-7.66(m，2H)，7.19(d，J＝7.9Hz，1H)，6.78-6.89(m，2H)，4.67-4.71(m，4H)，3.15-3.26(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 339(M+H)+。
Example 275
5- (hydroxymethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
A solution of calcium chloride (0.031g, 0.277mmol) in ethanol (0.8mL) was added to a suspension of methyl 2- (4- (propylcarbamoyl) phenylcarbamoyl) isoindoline-5-carboxylate (0.04g, 0.105mmol) in tetrahydrofuran (1 mL). Sodium borohydride (0.02g, 0.524mmol) was then added in one portion and the suspension was stirred at room temperature. After 18 hours, the mixture was concentrated to remove tetrahydrofuran, and then saturated aqueous sodium bicarbonate solution and water were added. Filtering the suspension and subjecting the solid to flash chromatography to provide The title compound.1HNMR(300MHz，DMSO-d6)δppm 8.55(s，1H)，8.25(t，J＝5.6Hz，1H)，7.74-7.78(m，2H)，7.64-7.67(m，2H)，7.31(d，J＝4.0Hz，1H)，7.30(d，J＝2.3Hz，1H)，7.26(d，J＝8.0Hz，1H)，5.19(t，J＝5.6Hz，1H)，4.71-4.78(m，4H)，4.52(d，J＝5.4Hz，2H)，3.15-3.25(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 354(M+H)+。
Example 276
5- (aminomethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
In a 50mL pressure bottle, 5-cyano-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide (0.04g, 0.115mmol) and 7M ammonia-methanol/tetrahydrofuran/methanol (4mL) were added to an aqueous slurry of Ra-Ni 2800 (0.080g, 1.363mmol) and stirred at 30psi and room temperature for 16 hours. The mixture was filtered through a nylon membrane, concentrated, and purified by reverse phase HPLC to provide the title compound.1H NMR (300MHz, methanol-d4)δppm 7.76-7.79(m，2H)，7.60-7.63(m，2H)，7.31-7.35(m，3H)，4.82(s，4H)，3.86(s，2H)，3.30-3.33(m，2H)，1.53-1.75(m，2H)，0.98(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 425(M+H)+。
Example 277
5- [ (2-hydroxy-2-methylpropanoyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and 2-hydroxy-2-methylpropionic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 9.59(s，1H)，8.55(s，1H)，8.25(t，J＝5.7Hz，1H)，7.81(s，1H)，7.74-7.78(m，2H)，7.62-7.68(m，2H)，7.59-7.64(m，1H)，7.28(d，J＝8.3Hz，1H)，5.71-5.75(m，1H)，4.72-4.80(m，4H)，3.16-3.23(m，2H)，1.42-1.59(m，2H)，1.36(s，6H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 425(M+H)+。
Example 278
5-acetamido-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
A solution of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide (0.035g, 0.103mmol) in dimethylformamide (0.7mL) was treated with N, N-diisopropylethylamine (0.018mL, 0.103mmol) followed by acetyl chloride (0.011g, 0.134mmol) and the reaction solution was stirred at room temperature for 16 hours. The reaction was concentrated and purified by reverse phase HPLC to provide the title compound. 1H NMR(300MHz，DMSO-d6)δppm9.97(s，1H)，8.52(s，1H)，8.25(t，J＝5.7Hz，1H)，7.74-7.78(m，2H)，7.65-7.67(m，1H)，7.62-7.67(m，2H)，7.43(dd，J＝8.2，1.9Hz，1H)，7.27(d，J＝8.2Hz，1H)，4.71-4.76(m，4H)，3.16-3.21(m，2H)，2.04(s，3H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e381(M+H)+。
Example 279
5- [ (N, N-dimethylglycyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and 2- (dimethylamino) acetic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 9.76(s，1H)，8.54(s，1H)，8.25(t，J＝5.6Hz，1H)，7.74-7.78(m，2H)，7.73(d，J＝1.8Hz，1H)，7.63-7.67(m，2H)，7.54(dd，J＝8.2，1.9Hz，1H)，7.28(d，J＝8.2Hz，1H)，4.72-4.76(m，4H)，3.16-3.24(m，2H)，3.07(s，2H)，2.28(s，6H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(-))m/e 422(M-H)-。
Example 280
N- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
In a 4mL vial, a solution of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide (50mg, 0.12mmol) and 1H-pyrazol-3-ylboronic acid (17mg, 0.15mmol) in dimethylformamide was treated with saturated aqueous sodium bicarbonate solution, followed by bis (triphenylphosphine) palladium (II) chloride (7 mg). The vial was capped under nitrogen and the reaction was heated at 85 ℃ for 6 hours. The reaction was cooled to ambient temperature and water was added. The resulting suspension was stirred for 5 minutes and filtered. Washing the collected solid with water and vacuum drying; the solid was purified by reverse phase HPLC to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm12.39-13.18(bs，1H)，8.59(s，1H)，8.24-8.28(m，1H)，7.75-7.79(m，2H)，7.70-7.80(m，3H)，7.62-7.69(m，2H)，7.40(d，J＝7.9Hz，1H)，6.73(d，J＝2.2Hz，1H)，4.79-4.83(m，4H)，3.15-3.25(m，2H)，1.46-1.57(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 390(M+H)+。
Example 281
N- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280 with 4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole instead of 1H-pyrazol-3-ylboronic acid.1HNMR(300MHz，DMSO-d6)δppm 10.91-13.69(bs，1H)，8.58(s，1H)，8.26(t，J＝5.7Hz，1H)，8.07-8.08(bs，2H)，7.75-7.79(m，2H)，7.67(s，1H)，7.54-7.65(m，2H)，7.57(d，J＝7.8Hz，1H)，7.34(d，J＝7.8Hz，1H)，4.76-4.79(m，4H)，3.15-3.25(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 390(M+H)+。
Example 282
5- [ (methoxyacetyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting 2-methoxyacetyl chloride for acetyl chloride.1H NMR(300MHz，DMSO-d6)δppm 9.80(s，1H)，8.54(s，1H)，8.25(t，J＝5.7Hz，1H)，7.74-7.79(m，2H)，7.72-7.74(m，1H)，7.63-7.67(m，2H)，7.55(dd，J＝8.2，1.9Hz，1H)，7.30(d，J＝8.2Hz，1H)，4.72-4.77(m，4H)，4.00(s，2H)，3.38(s，3H)，3.17-3.19(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 411(M+H)+。
Example 283
5- [ (methylsulfonyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
A solution of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide (0.035g, 0.103mmol), pyridine (0.017mL, 0.207mmol), and a catalytic amount of N, N-dimethylaminopyridine in dimethylformamide (0.7mL) was cooled to 0 ℃. Methanesulfonyl chloride (0.014g, 0.126mmol) was added, and the reaction solution was stirred at room temperature for 2 hours. The reaction mixture was concentrated and purified by reverse phase HPLC to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 9.74(s，1H)，8.54(s，1H)，8.26(t，J＝5.6Hz，1H)，7.74-7.78(m，2H)，7.63-7.66(m，2H)，7.32(d，J＝8.1Hz，1H)，7.14-7.20(m，2H)，4.73-4.76(m，4H)，3.15-3.25(m，2H)，2.98(s，3H)，1.45-1.62(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 417(M+H)+。
Table 4.
The following examples are prepared essentially as in example 1, substituting 1, 3-dihydro-2H-pyrrolo [3, 4-C ] pyridine, 5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine, or 6, 7-dihydro-5H-pyrrolo [3, 4-d ] pyrimidine for isoindoline in example 1A, using the appropriate amine described in example 1C. Some products were purified by flash chromatography while others were purified by reverse phase HPLC; some compounds also require Boc-deprotection after amide coupling as described in example 2D. Accordingly, some of the examples were isolated as trifluoroacetate salts.
Example 293
N- {4- [ (4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 293A
N- (4-nitrophenyl) isoindoline-2-carboxamide
A solution of N- (4-aminophenyl) isoindoline-2-carboxamide (100mg, 0.395mmol), 4-phenylbutyric acid (78mg, 0.474mmol), 1-hydroxybenzotriazole hydrate (66.5mg, 0.434mmol) and N-methylmorpholine (0.109mL, 0.987mmol) in N, N-dimethylformamide (1.771mL) was treated with N- (3-dimethylaminopropyl) -N' -ethylcarbodiimide hydrochloride (136mg, 0.711mmol) at room temperature. The mixture was stirred overnight, diluted with water (10 ml); the resulting suspension was filtered, washed with water and dried to obtain a product containing impurities. The solid was suspended in 2% methanol/dichloromethane and filtered to provide the title compound.
Example 293B
N- (4-aminophenyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 274 using N- (4-nitrophenyl) isoindoline-2-carboxamide instead of 5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxamide.
Example 293C
N- {4- [ (4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
A solution of N- (4-aminophenyl) isoindoline-2-carboxamide (100mg, 0.395mmol), 4-phenylbutyric acid (78mg, 0.474mmol), 1-hydroxybenzotriazole hydrate (66.5mg, 0.434mmol) and N-methylmorpholine (0.109mL, 0.987mmol) in dimethylformamide (1.771mL) was treated with N- (3-dimethylaminopropyl) -N' -ethylcarbodiimide hydrochloride (136mg, 0.711mmol) at room temperature. The mixture was stirred overnight, diluted with water (10 ml); the resulting suspension was filtered and washed with water to obtain a product containing impurities. The solid was suspended in 2% methanol/dichloromethane and filtered to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 1.78-2.00(m，2H)，2.30(t，J＝7.3Hz，2H)，2.62(t，J＝7.5Hz，2H)，4.75(s，4H)，7.08-7.41(m，9H)，7.46(s，4H)，8.26(s，1H)，9.73(s，1H)；(ESI(+))m/e 400(M+H)+。
Table 5.
The following examples are prepared essentially as described in example 293, substituting the appropriate amine in example 293A and the appropriate carboxylic acid for 4-phenylbutyric acid in example 293C. Some products were purified by flash chromatography while others were purified by reverse phase HPLC; accordingly, some of the examples were isolated as trifluoroacetate salts.
Example 313
2- ({4- [ (Cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid methyl ester
Example 313A
2- (4-Nitrophenylcarbamoyl) isoindoline-5-carboxylic acid methyl ester
The title compound was prepared as described in example 1A substituting 4-nitrophenyl isocyanate for methyl 4-isocyanatobenzoate and methyl isoindoline-5-carboxylate hydrochloride for isoindoline.
Example 313B
2- (4-Aminophenylcarbamoyl) isoindoline-5-carboxylic acid methyl ester
The title compound was prepared as described in example 274, substituting 2- (4-nitrophenylcarbamoyl) isoindoline-5-carboxylic acid methyl ester for 5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxamide.
Example 313C
2- ({4- [ (Cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid methyl ester
The title compound was prepared as described in example 278, substituting 2- (4-aminophenylcarbamoyl) isoindoline-5-carboxylic acid methyl ester for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide and 2-cyclopentylacetyl chloride for acetyl chloride.1H NMR(300MHz，DMSO-d6)δppm 9.69(s，1H)，8.32(s，1H)，7.94-7.94(m，1H)，7.89-7.96(m，1H)，7.51(d，J＝8.1Hz，1H)，7.41-7.49(m，4H)，4.75-4.82(m，4H)，3.87(s，3H)，2.24-2.29(m，2H)，2.15-2.28(m，1H)，1.68-1.81(m，2H)，1.44-1.67(m，4H)，1.13-1.24(m，2H)；MS(ESI(+))m/e 422(M+H)+。
Example 314
2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid
The title compound was prepared as described in example 1B, using 2- ({4- [ (cyclopentylacetyl) amino]Phenyl } carbamoyl) isoindoline-5-carboxylic acid methyl ester instead of 4- (isoindoline-2-carboxamido) benzoic acid methyl ester. 1H NMR(300MHz，DMSO-d6)δppm12.97(dd，J＝4.1，2.1Hz，1H)，9.70(s，1H)，8.32(s，1H)，7.88-7.92(m，2H)，7.46-7.50(m，1H)，7.43-7.48(m，4H)，4.79-4.81(bs，4H)，2.24-2.30(m，2H)，2.16-2.29(m，1H)，1.68-1.81(m，2H)，1.44-1.67(m，4H)，1.10-1.27(m，2H)；MS(ESI(-))m/e 406(M-H)-。
Example 315
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
To a stirred suspension of 2- (4- (2-cyclopentylacetamido) phenylcarbamoyl) isoindoline-5-carboxylic acid (18mg, 0.044mmol) in tetrahydrofuran was added dropwise 1M borane/tetrahydrofuran (0.18ml, 0.18 mmol). The mixture was heated at 60 ℃ for 1 hour. The reaction was cooled to room temperature, treated with a few drops of 4M HCl-dioxane and methanol, and the clear solution was stirred at room temperature for 2 hours. The reaction was concentrated and purified by reverse phase HPLC to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 9.69(s，1H)，8.26(s，1H)，7.45(s，4H)，7.28-7.32(m，2H)，7.22-7.26(m，1H)，5.18-5.22(m，1H)，4.72-4.73(bs，4H)，4.50-4.53(bs，2H)，2.17-2.32(m，3H)，1.70-1.80(m，2H)，1.44-1.67(m，4H)，1.13-1.24(m，2H)；MS(ESI(+))m/e394(M+H)+。
Example 316
N- {4- [ (2-Cyclopentylethyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
To a stirred suspension of 2- (4- (2-cyclopentylacetamido) phenylcarbamoyl) isoindoline-5-carboxylic acid (18mg, 0.044mmol) in tetrahydrofuran was added dropwise 1M borane/tetrahydrofuran (0.18ml, 0.18 mmol). The mixture is added at 6Heating at 0 deg.C for 1 hr. The reaction was cooled to room temperature, treated with a few drops of 4M HCl-dioxane and methanol, and the clear solution was stirred at room temperature for 2 hours. The reaction was concentrated and purified by reverse phase HPLC to provide the title compound. 1H NMR(300MHz，DMSO-d6)δppm 7.92(s，1H)，7.27-7.31(m，2H)，7.24(d，J＝8.1Hz，1H)，7.15-7.20(m，2H)，6.45-6.51(m，2H)，5.17-5.21(m，2H)，4.68-4.69(bs，4H)，4.51(d，J＝5.4Hz，2H)，2.97(q，J＝6.7Hz，2H)，1.70-1.95(m，3H)，1.42-1.66(m，6H)，1.04-1.20(m，2H)；MS(ESI(+))m/e 380(M+H)+。
Example 317
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester
Example 317A
N- (4-bromophenyl) isoindoline-2-carboxamide
The title compound was prepared as described in example 1A substituting 4-bromophenyl isocyanate for methyl 4-isocyanatobenzoate.
Example 317B
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester
The title compound was prepared as described in example 280, substituting 4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester for 1H-pyrazol-3-ylboronic acid and N- (4-bromophenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6)δppm 8.38(s，1H)，7.55-7.57(m，2H)，7.26-7.42(m，6H)，6.06-6.09(bs，1H)，4.76-4.77(bs，4H)，3.97-4.00(m，2H)，3.51-3.55(m，2H)，2.42-2.46(m，2H)，1.43(s，9H)；MS(ESI(-))m/e418(M-H)-。
Example 318
N- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 2D using 4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino]Phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester instead of 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamic acid tert-butyl ester. 1H NMR(400MHz，DMSO-d6)δppm 8.44(s，1H)，7.58-7.61(m，2H)，7.30-7.41(m，6H)，6.12-6.14(bs，1H)，4.77-4.78(bs，4H)，3.70-3.72(m，2H)，3.27-3.31(m，2H)，2.60-2.64(m，2H)；MS(ESI(+))m/e 320(M+H)+。
Example 319
N- {4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280 with 1-isopentyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole instead of 1H-pyrazol-3-ylboronic acid and N- (4-bromophenyl) isoindoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm0.91(d，J＝6.4Hz，6H)，1.40-1.60(m，1H)，1.70(q，J＝6.8Hz，2H)，4.11(t，J＝7.1Hz，2H)，4.77(s，4H)，7.13-7.40(m，4H)，7.42-7.50(m，2H)，7.50-7.61(m，2H)，7.78(s，1H)，8.08(s，1H)，8.32(s，1H)；MS(ESI(+))m/e 375(M+H)+。
Example 320
N- [4- (1-methyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280 with 1-methyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole instead of 1H-pyrazol-3-ylboronic acid, N- (4-bromophenyl) isoIndoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm3.84(s，3H)，4.77(s，4H)，7.24-7.40(m，4H)，7.40-7.49(m，2H)，7.50-7.60(m，2H)，7.77(s，1H)，8.02(s，1H)，8.33(s，1H)；MS(ESI(+))m/e319(M+H)+。
Example 321
N- {4- [ (1E) -5-phenylpent-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280 with (E) -4, 4, 5, 5-tetramethyl-2- (5-phenylpent-1-enyl) -1, 3, 2-dioxaborolan substituting 1H-pyrazol-3-ylboronic acid and N- (4-bromophenyl) isoindoline-2-carboxamide substituting 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(300MHz，DMSO-d6)δppm1.60-1.84(m，2H)，2.19(q，J＝7.0Hz，2H)，2.55-2.71(m，2H)，4.76(s，4H)，6.12-6.27(m，1H)，6.26-6.43(m，1H)，7.09-7.44(m，11H)，7.52(d，J＝8.5Hz，2H)，8.33(s，1H)；MS(ESI(+))m/e 383(M+H)+。
Example 322
N- [4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting 1-propyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N- (4-bromophenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 0.85(t，J＝7.3Hz，3H)，1.69-1.93(m，2H)，4.05(t，J＝6.9Hz，2H)，4.77(s，4H)，7.26-7.40(m，4H)，7.42-7.49(m，2H)，7.52-7.61(m，2H)，7.79(s，1H)，8.07(s，1H)，8.33(s，1H)；MS(ESI(+))m/e 347(M+H)+。
Example 323
N- [4- (1-benzyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting 1-benzyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N- (4-bromophenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm4.77(s，4H)，5.33(s，2H)，7.21-7.42(m，9H)，7.41-7.51(m，2H)，7.51-7.61(m，2H)，7.84(s，1H)，8.17(s，1H)，8.33(s，1H)；MS(ESI(+))m/e395(M+H)+。
Example 324
N- {4- [1- (2-hydroxyethyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting 2- (4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazol-1-yl) ethanol for 1H-pyrazol-3-ylboronic acid and N- (4-bromophenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(300MHz，DMSO-d6)δppm3.76(q，J＝5.8Hz，2H)，4.14(t，J＝5.6Hz，2H)，4.77(s，4H)，4.90(t，J＝5.4Hz，1H)，7.25-7.41(m，4H)，7.41-7.51(m，2H)，7.51-7.60(m，2H)，7.80(s，1H)，8.04(s，1H)，8.32(s，1H)；MS(ESI(+))m/e 349(M+H)+。
Example 325
N- [6- (1-propyl-1H-pyrazol-4-yl) pyridin-3-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 325A
N- (6-chloropyridin-3-yl) isoindoline-2-carboxamide
The title compound was prepared as described in example 1A, substituting 2-chloro-5-isocyanatopyridine for methyl 4-isocyanatobenzoate.
Example 325B
N- [6- (1-propyl-1H-pyrazol-4-yl) pyridin-3-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280 with 1-propyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole instead of 1H-pyrazol-3-ylboronic acid and N- (6-chloropyridin-3-yl) isoindoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm8.90-8.92(bs，1H)，8.84(d，J＝2.5Hz，1H)，8.39(s，1H)，8.25(dd，J＝8.8，2.5Hz，1H)，8.08(s，1H)，7.87(d，J＝8.8Hz，1H)，7.31-7.41(m，4H)，4.79-4.83(bs，4H)，4.13(t，J＝6.9Hz，2H)，1.77-1.89(m，2H)，0.86(t，J＝7.3Hz，3H)；MS(ESI(+))m/e 348(M+H)+。
Example 326
N- {6- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280 with 1-isopentyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole instead of 1H-pyrazol-3-ylboronic acid and N- (6-chloropyridin-3-yl) isoindoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(300MHz，DMSO-d6)δppm 8.85-8.87(bs，1H)，8.81(d，J＝2.5Hz，1H)，8.38(s，1H)，8.21(dd，J＝8.8，2.5Hz，1H)，8.05(s，1H)，7.82(d，J＝8.8Hz，1H)，7.31-7.41(m，4H)，4.78-4.83(bs，4H)，4.19(t，J＝7.1Hz，2H)，1.71(q，J＝7.0Hz，2H)，1.40-1.59(m，1H)，0.92(d，J＝6.6Hz，6H)；MS(ESI(-))m/e374(M-H)-。
Example 327
N- [4- (5-phenylpentyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 274 using N- {4- [ (1E) -5-phenylpent-1-en-1-yl]Phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of 5-nitro-N- [4- (propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide.1H NMR(300MHz，DMSO-d6)δppm 1.21-1.40(m，4H)，1.49-1.67(m，4H)，2.45-2.62(m，2H)，4.75(s，4H)，7.05(d，J＝8.7Hz，2H)，7.14-7.40(m，9H)，7.44(d，J＝8.3Hz，2H)，8.23(s，1H)；MS(ESI(+))m/e 385(M+H)+。
Example 328
N- [ 2-fluoro-4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 328A
N- (4-bromo-2-fluorophenyl) isoindoline-2-carboxamide
The title compound was prepared as described in example 1A, substituting 4-bromo-2-fluoro-1-isocyanatobenzene for methyl 4-isocyanatobenzoate.
Example 328B
N- [ 2-fluoro-4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280 with 1-propyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole instead of 1H-pyrazol-3-ylboronic acid and N- (4-bromo-2-fluorophenyl) isoindoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm8.19(s，1H)，8.03(s，1H)，7.89(s，1H)，7.57(t，J＝8.4Hz，1H)，7.46(dd，J＝12.1，1.9Hz，1H)，7.24-7.39(m，5H)，4.76-4.78(bs，4H)，4.06(t，J＝6.9Hz，2H)，1.75-1.88(m，2H)，0.86(t，J＝7.3Hz，3H)；MS(ESI(+))m/e365(M+H)+。
Example 329
N- { 2-fluoro-4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280 with 1-isopentyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole instead of 1H-pyrazol-3-ylboronic acid and N- (4-bromo-2-fluorophenyl) isoindoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 8.21(s，1H)，8.04(s，1H)，7.88(s，1H)，7.56(t，J＝8.4Hz，1H)，7.46(dd，J＝12.1，1.9Hz，1H)，7.25-7.41(m，5H)，4.76-4.81(m，4H)，4.12(t，J＝7.2Hz，2H)，1.70(q，J＝7.1Hz，2H)，1.40-1.59(m，1H)，0.91(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 393(M+H)+。
Example 330
N- [4- (1-butanoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting butyryl chloride for acetyl chloride, N- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1HNMR(400MHz，DMSO-d6)δppm 8.38(s，1H)，7.55-7.58(m，2H)，7.27-7.38(m，6H)，6.09-6.11(m，1H)，4.77(s，4H)，4.08-4.14(m，2H)，3.58-3.68(m，2H)，2.39-2.51(m，2H)，2.34(dt，J＝19.8，7.3Hz，2H)，1.46-1.62(m，2H)，0.88-0.93(m，3H)；MS(ESI(+))m/e 390(M+H)+。
Example 331
N- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
As in the examples278 the title compound was prepared by substituting isobutyryl chloride for acetyl chloride, N- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1HNMR(500MHz，DMSO-d6)δppm 8.40(s，1H)，7.55-7.58(m，2H)，7.30-7.38(m，6H)，6.11-6.13(bs，1H)，4.76-4.77(bs，4H)，4.19-4.21(m，1H)，4.08-4.09(m，1H)，3.65-3.72(m，2H)，2.85-3.00(m，1H)，2.40-2.56(m，2H)，1.00-1.07(m，6H)；MS(ESI(+))m/e 390(M+H)+。
Example 332
N- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride, N- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1HNMR(400MHz，DMSO-d6)δppm 8.39(s，1H)，7.56-7.59(m，2H)，7.44-7.49(m，5H)，7.34-7.40(m，4H)，7.29-7.34(m，2H)，5.91-6.27(m，1H)，4.76-4.77(bs，4H)，4.02-4.26(m，2H)，3.36-3.59(m，2H)，2.51-2.61(m，2H)；MS(ESI(+))m/e 424(M+H)+。
Example 333
N- {4- [1- (isopropylsulfonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 283, substituting propane-2-sulfonyl chloride for methanesulfonyl chloride, N- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6)δppm 8.38-8.40(m，1H)，7.56-7.59(m，2H)，7.29-7.38(m，6H)，6.11-6.14(m，1H)，4.76-4.80(m，4H)，3.93-3.96(m，2H)，3.49(t，J＝5.5Hz，2H)，3.35-3.45(m，1H)，2.47-2.51(m，2H)，1.24(d，J＝6.9Hz，6H)；MS(ESI(-))m/e 424(M-H)-。
Example 334
N- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 334A
4- (5- (isoindoline-2-carboxamido) pyridin-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester
The title compound was prepared as described in example 280, using tert-butyl 4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylate instead of 1H-pyrazol-3-ylboronic acid and N- (6-chloropyridin-3-yl) isoindoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.
Example 334B
N- (6- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-3-yl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D, substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (5- (isoindoline-2-carboxamido) pyridin-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylate.
Example 334C
4- (5- (isoindoline-2-carboxamido) pyridin-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester
The title compound was prepared as described in example 278, substituting isobutyryl chloride for acetyl chloride and N- (6- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-3-yl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ ppm 8.70(d, J ═ 2.6Hz, 1H), 8.33-8.37(m, 1H), 7.95(dd, J ═ 8.6, 2.6Hz, 1H), 7.44(d, J ═ 8.6Hz, 1H), 7.28-7.36(m, 4H), 6.54-6.56(m, 1H), 4.79(s, 4H), 4.16-4.18(m, 2H), 3.68(t, J ═ 5.7Hz, 2H), 2.86-2.97(m, 1H), 2.54-2.63(m, 2H), 1.04(d, J ═ 6.7Hz, 6H); MS (ESI (-)) M/e 389(M-H) -。
Example 335
N- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride and N- (6- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-3-yl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6)δppm 8.71(d，J＝2.5Hz，1H)，8.61(s，1H)，8.01(dd，J＝8.6，2.2Hz，1H)，7.42-7.54(m，6H)，7.35-7.39(m，2H)，7.29-7.35(m，2H)，6.46-6.67(m，1H)，4.79(s，4H)，4.05-4.32(m，2H)，3.77-3.94(m，1H)，3.47-3.58(m，1H)，2.61-2.65(m，2H)；MS(ESI(+))m/e 425(M+H)+。
Example 336
N- [4- (4-benzoylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 336A
N- (4- (piperazin-1-yl) phenyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D substituting 4- (4- (isoindoline-2-carboxamido) phenyl) piperazine-1-carboxylic acid tert-butyl ester for 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.
Example 336B
N- [4- (4-benzoylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride and N- (4- (piperazin-1-yl) phenyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(300MHz，DMSO-d6)δppm 8.14(s，1H)，7.38-7.50(m，7H)，7.28-7.38(m，4H)，6.87-6.91(m，2H)，4.74(s，4H)，3.39-3.90(m，4H)，3.01-3.17(m，4H)；MS(ESI(+))m/e427(M+H)+。
Example 337
N- {4- [4- (isopropylsulfonyl) piperazin-1-yl ] phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 283, substituting methanesulfonyl chloride with isopropylsulfonyl chloride and N- (4- (piperazin-1-yl) phenyl) isoindoline-2-carboxamide with 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 8.16(s，1H)，7.39-7.45(m，2H)，7.27-7.38(m，4H)，6.88-6.92(m，2H)，4.74(s，4H)，3.07-3.12(m，4H)，1.25(d，J＝6.8Hz，6H)；MS(ESI(+))m/e 429(M+H)+。
Example 338
N- {4- [4- (phenylsulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 283, substituting benzenesulfonyl chloride for methanesulfonyl chloride and N- (4- (piperazin-1-yl) phenyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 8.14(s，1H)，7.65-7.80(m，5H)，7.35-7.41(m，2H)，7.27-7.37(m，4H)，6.81-6.85(m，2H)，4.72(s，4H)，3.09-3.15(m，4H)，2.99-3.04(m，4H)；MS(ESI(-))m/e 461(M-H)-。
Example 339
N- {4- [3- (benzoylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 339A
1- (4-Nitrophenyl) pyrrolidin-3-ylcarbamic acid tert-butyl ester
A solution of 1-fluoro-4-nitrobenzene (508mg, 3.6mmol) and tert-butyl pyrrolidin-3-ylcarbamate (671mg, 3.6mmoI) in N, N-dimethylformamide (7ml) was heated at 55 ℃ for 1.5 hours, followed by stirring at room temperature overnight. The reaction mixture was poured into water and the suspension was filtered, washed with water and dried to provide the title compound.
Example 339B
1- (4-aminophenyl) pyrrolidin-3-ylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 274, substituting (+/-) -1- (4-nitrophenyl) pyrrolidin-3-ylcarbamic acid tert-butyl ester for 5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxamide.
Example 339C
1- (4- (isoindoline-2-carboxamido) phenyl) pyrrolidin-3-ylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 272B substituting (+/-) -1- (4-aminophenyl) pyrrolidin-3-ylcarbamic acid tert-butyl ester for 4-amino-N-propylbenzamide and isoindoline for isoindoline-5-carboxylic acid methyl ester hydrochloride in example 272B.
Example 339D
N- [4- (3-Aminopyrrolidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 2, substituting (+/-) -1- (4- (isoindoline-2-carboxamido) phenyl) pyrrolidin-3-ylcarbamate for tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate in example 2D.
Example 339E
N- {4- [ (3R) -3- (benzoylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide and N- {4- [ (3S) -3- (benzoylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride, (+/-) -N- (4- (3-aminopyrrolidin-1-yl) phenyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 8.61(d，J＝6.8Hz，1H)，8.01(s，1H)，7.85-7.89(m，2H)，7.42-7.56(m，3H)，7.28-7.37(m，6H)，6.50(d，J＝8.7Hz，2H)，4.72(s，4H)，4.56-4.67(m，1H)，3.53-3.59(m，1H)，3.36-3.45(m，1H)，3.16-3.24(m，1H)，2.22-2.31(m，1H)，2.03-2.13(m，1H)；MS(ESI(+))m/e 427(M+H)+。
Example 340
N- {4- [ (3R) -3- (butyrylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide and N- {4- [ (3S) -3- (butyrylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting butyryl chloride for acetyl chloride.1H NMR(300MHz，DMSO-d6)δppm 8.06(d，J＝6.9Hz，1H)，7.28-7.37(m，6H)，6.47(d，J＝8.7Hz，2H)，4.72(s，4H)，4.36(h，J＝5.7Hz，1H)，3.41-3.47(m，1H)，3.17-3.23(m，1H)，2.89-3.05(m，1H)，2.10-2.28(m，1H)，2.05(t，J＝7.3Hz，2H)，1.81-1.96(m，1H)，1.45-1.58(m，2H)，0.85(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 393(M+H)+。
Example 341
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperazine-1-carboxylic acid tert-butyl ester
Example 341A
4- (4-Nitrophenyl) piperazine-1-carboxylic acid tert-butyl ester
A solution of 1-fluoro-4-nitrobenzene (500mg, 3.54mmol) and piperazine-1-carboxylic acid tert-butyl ester (726mg, 3.9mmol) in dimethylformamide was treated with potassium carbonate (735mg, 5.32mmol) and the suspension was heated at 55 ℃ for 4 hours and then stirred at room temperature overnight. The reaction was poured into water and the suspension was filtered, washed with water and dried under vacuum to provide the title compound.
Example 341B
4- (4-aminophenyl) piperazine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 274, substituting 4- (4-nitrophenyl) piperazine-1-carboxylic acid tert-butyl ester for 5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxamide.
Example 341C
4- (4- (isoindoline-2-carboxamido) phenyl) piperazine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272B substituting 4- (4-aminophenyl) piperazine-1-carboxylic acid tert-butyl ester for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm8.14(s，1H)，7.38-7.44(m，2H)，7.27-7.39(m，4H)，6.88-6.90(m，1H)，6.86(s，1H)，4.73(s，4H)，3.40-3.51(m，4H)，2.98-3.02(m，4H)，1.42(s，9H)；MS(ESI(-))m/e 421(M-H)-。
Example 342
N- [4- (4-propionylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting propionyl chloride for acetyl chloride and N- (4- (piperazin-1-yl) phenyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 8.14(s，1H)，7.38-7.44(m，2H)，7.28-7.39(m，4H)，6.87-6.90(m，2H)，4.74(s，4H)，3.54-3.60(m，4H)，2.95-3.10(m，4H)，2.36(q，J＝7.4Hz，2H)，1.03(s，1H)，1.00(d，J＝7.4Hz，2H)；MS(ESI(+))m/e 379(M+H)+。
Example 343
N- {4- [4- (cyclopropylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting cyclopropanecarbonyl chloride for acetyl chloride and N- (4- (piperazin-1-yl) phenyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(300MHz，DMSO-d6)δppm 8.15(s，1H)，7.38-7.45(m，2H)，7.28-7.39(m，4H)，6.87-6.93(m，2H)，4.74(s，4H)，3.73-3.90(m，2H)，3.50-3.70(m，2H)，3.02-3.18(m，4H)，1.98-2.07(m，1H)，0.68-0.77(m，4H)；MS(ESI(-))m/e 389(M-H)-。
Example 344
N- (2-butanoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 344A
5- (isoindoline-2-carboxamido) isoindoline-2-carboxylic acid tert-butyl ester
Triphosgene (234mg, 0.790mmol) was mixed with anhydrous dichloromethane (25ml) in a 250ml round bottom flask at room temperature. To this solution was added dropwise a slurry of tert-butyl 5-aminoisoindoline-2-carboxylate (500mg, 2.134mmol) and diisopropylethylamine (0.410ml, 2.347mmol) in dry dichloromethane (20ml) over 15 minutes. The mixture was stirred at room temperature overnight. A solution of isoindoline (0.242ml, 2.134mmol) and diisopropylethylamine (0.410ml, 2.347mmol) in dry dichloromethane (20ml) was added in one portion. The reaction was stirred at room temperature overnight. The solvent was removed and the residue was purified by normal phase flash chromatography to afford the title compound.
Example 344B
N- (isoindolin-5-yl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D, substituting tert-butyl 5- (isoindoline-2-carboxamido) isoindoline-2-carboxylate for tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.
Example 344C
N- (2-butanoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting butyryl chloride for acetyl chloride and N- (isoindolin-5-yl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6)δppm 8.39(s，1H)，7.59-7.61(bs，1H)，7.43-7.48(m，1H)，7.30-7.41(m，4H)，7.22(t，J＝7.7Hz，1H)，4.77(d，J＝13.9Hz，2H)，4.77(s，4H)，4.55-4.60(m，2H)，2.33(td，J＝7.3，3.7Hz，2H)，1.54-1.63(m，2H)，0.93(td，J＝7.3，1.4Hz，3H)；MS(ESI(+))m/e 350(M+H)+。
Example 345
N- (2-isobutyryl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting isobutyryl chloride for acetyl chloride, N- (isoindolin-5-yl) isoindoline-2-carboxamideInstead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6)δppm 8.40(s，1H)，7.59-7.61(bs，1H)，7.46(ddd，J＝10.8，8.5，2.1Hz，1H)，7.30-7.38(m，4H)，7.20-7.24(m，1H)，4.82-4.87(m，2H)，4.76-4.77(bs，4H)，4.55-4.60(m，2H)，2.78(h，J＝6.9Hz，1H)，1.07(d，J＝6.7Hz，6H)；MS(ESI(+))m/e 350(M+H)+。
Example 346
N- (2-benzoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride and N- (isoindolin-5-yl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6)δppm 8.40(d，J＝8.8Hz，1H)，7.59-7.67(m，3H)，7.11-7.52(m，9H)，4.68-4.84(m，8H)；MS(ESI(+))m/e 384(M+H)+。
Example 347
N- [2- (3-methylbutyl) -2, 3-dihydro-1H-isoindol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 429 with 3-methylbutanal instead of isobutyraldehyde and N- (isoindolin-5-yl) isoindoline-2-carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6)δppm 8.28(s，1H)，7.47(s，1H)，7.29-7.37(m，5H)，7.09(d，J＝8.1Hz，1H)，4.75(s，4H)，3.77-3.79(m，2H)，3.74-3.76(m，2H)，2.64(t，J＝7.5Hz，2H)，1.60-1.71(m，1H)，1.37-1.43(m，2H)，0.91(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 350(M+H)+。
Example 348
N- [4- (hexyloxy) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting 1- (hexyloxy) -4-isocyanatobenzene for methyl 4-isocyanatobenzoate.1H NMR(300MHz，DMSO-d6)δppm8.17(s，1H)，7.39-7.45(m，2H)，7.27-7.39(m，4H)，6.81-6.85(m，2H)，4.74(s，4H)，3.91(t，J＝6.5Hz，2H)，1.64-1.73(m，2H)，1.35-1.47(m，2H)，1.23-1.38(m，4H)，0.85-0.91(m，3H)；MS(ESI(+))m/e 339(M+H)+。
Example 349
N- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride, N- [4- (piperidin-4-yl) butyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6) δ ppm 7.39-7.47(m, 3H)7.22-7.40(m, 6H)6.27(t, J ═ 5.43Hz, 1H)4.56(s, 4H)4.36-4.52(br s, 1H)3.52(br s, 1H)3.00-3.15(m, 2H)2.93(br s, 1H)0.93-1.86 (br m, 12H series); MS (ESI (+)) M/e 406(M + H)+。
Example 350
N- {4- [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting nicotinoyl chloride hydrochloride for acetyl chloride, N- [4- (piperidin-4-yl) butyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6) δ ppm 8.58-8.71(m, 2H)7.87(d, J ═ 7.5Hz, 1H)7.52(dd, J ═ 7.5, 4.8Hz, 1H)7.22-7.36(m, 4H)6.28(br m, 1H)4.56(s, 4H)4.44(br m, 1H)3.38-3.57(br m, 1H)2.95-3.15(br m, 2H)2.68-2.84(brm, 1H)0.95-1.84(br, m, 12H of the series); MS (ESI (+)) m/e407(M+H)+。
Example 351
N- [6- (4-chlorophenoxy) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 344A, substituting 6- (4-chlorophenoxy) hex-1-amine for tert-butyl 5-aminoisoindoline-2-carboxylate.1H NMR(300MHz，DMSO-d6)δppm 1.40(q，6H)，1.70(q，2H)，3.08(q，J＝6.8Hz，2H)，3.95(t，J＝6.4Hz，2H)，4.57(s，4H)，6.27(t，J＝5.4Hz，1H)，6.85-7.01(m，2H)，7.21-7.39(m，6H)；MS(ESI(+))m/e 373(M+H)+。
Example 352
N- [4- (piperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 352A
4- (4- (isoindoline-2-carboxamido) butyl) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 344, substituting 4- (4-aminobutyl) piperidine-1-carboxylic acid tert-butyl ester for 5-aminoisoindoline-2-carboxylic acid tert-butyl ester in example 344A.
Example 352B
N- [4- (piperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 2D substituting 4- (4- (isoindoline-2-carboxamido) butyl) piperidine-1-carboxylic acid tert-butyl ester for 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.1H NMR(300MHz，DMSO-d6)δppm 1.14-1.34(m，6H)，1.35-1.57(m，3H)，1.76(d，J＝12.30Hz，2H)，2.69-2.89(m，2H)，3.07(q，J＝6.74Hz，2H)，3.21(d，J＝12.70Hz，2H)，4.57(s，4H)，6.29(t，J＝5.55Hz，1H)，7.11-7.41(m，4H)，8.31(s，1H)；MS(ESI(+))m/e 299(M+H)+。
Example 353
N, N' -Hexane-1, 6-diylbis (1, 3-dihydro-2H-isoindole-2-carboxamide)
The title compound was prepared as described in example 1A, substituting 1, 6-diisocyanatohexane for methyl 4-isocyanatobenzoate.1H NMR(300MHz，DMSO-d6)δppm7.19-7.37(m，8H)6.28(t，J＝5.59Hz，2H)4.57(s，8H)3.07(q，J＝6.8Hz，4H)1.37-1.55(m，4H)1.21-1.37(m，4H)；MS(ESI(+))m/e 407(M+H)+。
Example 354
N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting (4-isocyanatobutyl) benzene for methyl 4-isocyanatobenzoate.1H NMR(300MHz，DMSO-d6)δppm7.24-7.33(m，6H)，7.13-7.22(m，3H)，6.30(t，J＝5.6Hz，1H)，4.56(s，4H)，3.06-3.13(m，2H)，2.59(t，J＝7.4Hz，2H)，1.51-1.65(m，2H)，1.40-1.53(m，2H)；MS(ESI(+))m/e 295(M+H)+。
Example 355
6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] hexanoic acid ethyl ester
The title compound was prepared as described in example 1A, substituting ethyl 6-isocyanatohexanoate for methyl 4-isocyanatobenzoate.1H NMR(300MHz，DMSO-d6)δppm7.25-7.33(m，4H)，6.29(t，J＝5.6Hz，1H)，4.57(s，4H)，4.04(q，J＝7.1Hz，2H)，3.02-3.09(m，2H)，2.28(t，J＝7.3Hz，2H)，1.48-1.60(m，2H)，1.39-1.50(m，2H)，1.23-1.34(m，2H)，1.16(t，J＝7.1Hz，3H)；MS(ESI(+))m/e 305(M+H)+。
Example 356
N-hexyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting 1-isocyanatohexane for methyl 4-isocyanatobenzoate. 1H NMR(300MHz，DMSO-d6)δppm7.25-7.33(m，4H)，6.27(t，J＝5.6Hz，1H)，4.57(s，4H)，3.02-3.10(m，2H)，1.36-1.51(m，2H)，1.25-1.30(m，6H)，0.81-0.92(m，3H)；MS(ESI(-))m/e 245(M-H)-。
Example 357
N- (3-phenylpropyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting (3-isocyanatopropyl) benzene for methyl 4-isocyanatobenzoate.1H NMR(300MHz，DMSO-d6)δppm7.11-7.37(m，9H)，6.31(t，J＝5.5Hz，1H)，4.57(s，4H)，3.07-3.14(m，2H)，2.60(t，J＝7.6Hz，2H)，1.71-1.81(m，2H)；MS(ESI(+))m/e281(M+H)+。
Example 358
N-octyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting 1-isocyanatooctane for methyl 4-isocyanatobenzoate.1H NMR(300MHz，DMSO-d6)δppm7.24-7.35(m，4H)，6.27(t，J＝5.5Hz，1H)，4.57(s，4H)，3.02-3.09(m，2H)，1.40-1.47(m，2H)，1.25-1.27(m，10H)，0.81-0.89(m，3H)；MS(ESI(+))m/e 275(M+H)+。
Example 359
N- {6- [ (1-methyl-1H-pyrazol-4-yl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 359A
6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] hexanoic acid
The title compound was prepared as described in example 1B substituting ethyl 6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] hexanoate for methyl 4- (isoindoline-2-carboxamido) benzoate.
Example 359B
N- {6- [ (1-methyl-1H-pyrazol-4-yl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 1-methyl-1H-pyrazol-4-amine for 3-phenylpropan-1-amine, 6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino]Hexanoic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid. 1H NMR(300MHz，DMSO-d6)δppm 9.81(s，1H)，7.82(s，1H)，7.34-7.36(m，1H)，7.24-7.34(m，4H)，6.28(t，J＝5.5Hz，1H)，4.56(s，4H)，3.75(s，3H)，3.03-3.10(m，2H)，2.22(t，J＝7.3Hz，2H)，1.51-1.64(m，2H)，1..0-1.52(m，2H)，1.23-1.34(m，2H)；MS(ESI(+))m/e 356(M+H)+。
Example 360
N- [6- (methylamino) -6-oxohexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting methylamine for 3-phenylprop-1-amine, 6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino]Hexanoic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 7.60-7.72(m，1H)，7.25-7.33(m，4H)，6.24-6.29(m，1H)，4.57(s，4H)，2.94-3.09(m，2H)，2.54(d，J＝4.6Hz，3H)，2.30(t，J＝7.3Hz，1H)，2.04(t，J＝7.4Hz，1H)，1.37-1.58(m，4H)，1.18-1.35(m，2H)；MS(ESI(+))m/e 290(M+H)+。
Example 361
N- { 6-oxo-6- [ (3-phenylpropyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, using 6- [ (1, 3-dihydro-2H-iso-isomer)Indol-2-ylcarbonyl) amino]Hexanoic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1HNMR(300MHz，DMSO-d6)δppm 7.75-7.80(m，1H)，7.24-7.34(m，6H)，7.12-7.22(m，3H)，6.27(t，J＝5.5Hz，1H)，4.56(s，4H)，2.98-3.11(m，4H)，2.52-2.58(m，2H)，2.06(t，J＝7.3Hz，2H)，1.62-1.72(m，2H)，1.37-1.58(m，4H)，1.12-1.33(m，2H)；MS(ESI(+))m/e 394(M+H)+。
Example 362
N- {6- [ (3-methylbutyl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine, 6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino]Hexanoic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm7.64-7.69(m，1H)，7.24-7.34(m，4H)，6.26(t，J＝5.5Hz，1H)，4.57(s，4H)，2.99-3.10(m，4H)，2.03(t，J＝7.3Hz，2H)，1.41-1.59(m，5H)，1.21-1.30(m，4H)，0.84(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 346(M+H)+。
Example 363
N- { 3-oxo-3- [ (3-phenylpropyl) amino ] propyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 363A
3- (isoindoline-2-carboxamido) propionic acid ethyl ester
The title compound was prepared as described in example 1A, substituting ethyl 3-isocyanatopropionate for methyl 4-isocyanatobenzoate.
Example 363B
3- (isoindoline-2-carboxamido) propionic acid
The title compound was prepared as described in example 1B, using ethyl 3- (isoindoline-2-carboxamido) propionate instead of methyl 4- (isoindoline-2-carboxamido) benzoate.
Example 363C
N- { 3-oxo-3- [ (3-phenylpropyl) amino ] propyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 3- (isoindoline-2-carboxamido) propionic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 7.87-7.92(m，1H)，7.22-7.32(m，6H)，7.12-7.19(m，3H)，6.36(t，J＝5.5Hz，1H)，4.56(s，4H)，3.24-3.32(m，2H)，3.03-3.10(m，2H)，2.52-2.60(m，2H)，2.30(t，J＝7.0Hz，2H)，1.63-1.74(m，2H)；MS(ESI(+))m/e 352(M+H)+。
Example 364
N- { 3-oxo-3- [4- (pyridin-2-yl) piperazin-1-yl ] propyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 1- (pyridin-2-yl) piperazine for 3-phenylpropan-1-amine and 3- (isoindoline-2-carboxamido) propionic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.11(ddd，J＝4.9，2.0，0.8Hz，1H)，7.53(ddd，J＝8.7，7.0，1.9Hz，1H)，7.25-7.34(m，4H)，6.83(d，J＝8.6Hz，1H)，6.65(ddd，J＝7.1，4.9，0.8Hz，1H)，6.37(t，J＝5.6Hz，1H)，4.57(s，4H)，3.44-3.61(m，8H)，3.28-3.37(m，2H)，2.54-2.61(m，2H)；MS(ESI(+))m/e 380(M+H)+。
Example 365
N- {3- [ (3-methylbutyl) amino ] -3-oxopropyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 13-methylbutan-1-amine for 3-phenylpropan-1-amine and 3- (isoindoline-2-carboxamido) propionic acid for 4- (isoindoline-2-carboxamido) benzoic acid. 1H NMR(300MHz，DMSO-d6)δppm7.76-7.81(m，1H)，7.25-7.34(m，4H)，6.31-6.36(m，1H)，4.56(s，4H)，3.23-3.31(m，2H)，3.02-3.09(m，2H)，2.27(t，J＝7.0Hz，2H)，1.46-1.62(m，1H)，1.27(q，J＝7.1Hz，2H)，0.84(d，J＝6.6Hz，6H)；MS(ESI(+))m/e304(M+H)+。
Example 366
N- [4- (1-propyl-1H-pyrazol-4-yl) benzyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 366A
N- (4-bromobenzyl) isoindoline-2-carboxamide
The title compound was prepared as described in example 1A, substituting 1-bromo-4- (isocyanatomethyl) benzene for methyl 4-isocyanatobenzoate.
Example 366B
N- [4- (1-propyl-1H-pyrazol-4-yl) benzyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting 1-propyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N- (4-bromobenzyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 0.85(t，J＝7.5Hz，3H)，1.70-1.92(m，2H)，4.06(t，J＝6.9Hz，2H)，4.29(d，J＝6.1Hz，2H)，4.63(s，4H)，6.91(t，J＝5.9Hz，1H)，7.18-7.40(m，6H)，7.49(d，J＝8.5Hz，2H)，7.82(s，1H)，8.12(s，1H)；MS(ESI(+))m/e361(M+H)+。
Example 367
N- [4- (1-isobutyl-1H-pyrazol-4-yl) benzyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, using 1-isobutyl-4- (4,4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole instead of 1H-pyrazol-3-ylboronic acid, and N- (4-bromobenzyl) isoindoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(300MHz，DMSO-d6)δppm0.86(d，J＝6.4Hz，6H)，2.03-2.21(m，1H)，3.91(d，J＝7.1Hz，2H)，4.28(d，J＝5.9Hz，2H)，4.63(s，4H)，6.92(t，J＝5.9Hz，1H)，7.25-7.37(m，6H)，7.50(d，J＝8.3Hz，2H)，7.83(s，1H)，8.10(s，1H)；MS(ESI(+))m/e375(M+H)+。
Example 368
N- (5- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (2-pyridyl) piperazine for 3-phenylpropan-1-amine and 6- (isoindoline-2-carboxamido) nicotinic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm 9.21(s，1H)，8.39(dd，J＝2.3，0.8Hz，1H)，8.13(dd，J＝4.9，1.9Hz，1H)，8.00(dd，J＝8.6，0.8Hz，1H)，7.84(dd，J＝8.6，2.4Hz，1H)，7.56(ddd，J＝8.7，6.9，1.9Hz，1H)，7.34-7.39(m，2H)，7.29-7.34(m，2H)，6.85(d，J＝8.5Hz，1H)，6.67(dd，J＝6.7，4.9Hz，1H)，4.75-4.92(bs，4H)，3.47-3.81(m，8H)；MS(ESI(+))m/e 429(M+H)+。
Example 369
N- {5- [ (3-phenylpropyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 369A
6- (isoindoline-2-carboxamido) nicotinic acid methyl ester
The title compound was prepared as described in example 344A substituting methyl 6-aminonicotinate for tert-butyl 5-aminoisoindoline-2-carboxylate.
Example 369B
6- (isoindoline-2-carboxamido) nicotinic acid
The title compound was prepared as described in example 1B substituting methyl 6- (isoindoline-2-carboxamido) nicotinate for methyl 4- (isoindoline-2-carboxamido) benzoate.
Example 369C
N- {5- [ (3-phenylpropyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 6- (isoindoline-2-carboxamido) nicotinic acid for 4- (isoindoline-2-carboxamido) benzoic acid. 1H NMR(400MHz，DMSO-d6)δppm 9.25(s，1H)，8.74(d，J＝2.4Hz，1H)，8.47-8.51(m，1H)，8.14(dd，J＝8.8，2.4Hz，1H)，8.00(d，J＝8.7Hz，1H)，7.33-7.38(m，2H)，7.29-7.33(m，2H)，7.26-7.30(m，2H)，7.21-7.26(m，2H)，7.15-7.21(m，1H)，4.74-4.92(bs，4H)，3.25-3.32(m，2H)，2.64(t，J＝7.6Hz，2H)，1.84(p，J＝7.4Hz，2H)；MS(ESI(+))m/e 401(M+H)+。
Example 370
N- {5- [ (3-methylbutyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 6- (isoindoline-2-carboxamido) nicotinic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm 9.24(s，1H)，8.73(d，J＝2.4Hz，1H)，8.42(t，J＝5.5Hz，1H)，8.13(dd，J＝8.8，2.4Hz，1H)，7.99(d，J＝8.7Hz，1H)，7.25-7.37(m，4H)，4.71-4.95(bs，4H)，3.24-3.32(m，2H)，1.57-1.68(m，1H)，1.43(q，J＝7.1Hz，2H)，0.91(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 353(M+H)+。
Example 371
N- {5- [ (3-phenylpropyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 371A
2- (isoindoline-2-carboxamido) thiazole-5-carboxylic acid methyl ester
The title compound was prepared as described in example 272B substituting 2-aminothiazole-5-carboxylic acid methyl ester for 4-amino-N-propylbenzamide and isoindoline for isoindoline-5-carboxylic acid methyl ester hydrochloride.
Example 371B
2- (isoindoline-2-carboxamido) thiazole-5-carboxylic acid
The title compound was prepared as described in example 1B, using methyl 2- (isoindoline-2-carboxamido) thiazole-5-carboxylate instead of methyl 4- (isoindoline-2-carboxamido) benzoate.
Example 371C
N- {5- [ (3-phenylpropyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 2- (isoindoline-2-carboxamido) thiazole-5-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid. 1HNMR(300MHz，DMSO-d6)δppm 11.00-11.19(bs，1H)，8.34(t，J＝5.6Hz，1H)，7.98(s，1H)，7.15-7.37(m，9H)，4.70-4.83(m，4H)，3.17-3.28(m，2H)，2.63(t，J＝7.6Hz，2H)，1.81(p，J＝7.4Hz，2H)；MS(ESI(-))m/e405(M-H)-。
Example 372
N- {5- [ (3-methylbutyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine2- (isoindoline-2-carboxamido) thiazole-5-carboxylic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm11.01-11.16(bs，1H)，8.27(t，J＝5.6Hz，1H)，7.96(s，1H)，7.29-7.36(m，4H)，4.73-4.88(bs，4H)，3.18-3.28(m，2H)，1.52-1.69(m，1H)，1.34-1.44(m，2H)，0.90(d，J＝6.6Hz，6H)；MS(ESI(-))m/e 357(M-H)-。
Example 374
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 374A
N- (4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) phenyl) isoindoline-2-carboxamide
500mg (4-isocyanatophenyl) boronic acid pinacol ester (1.979mmol) and 365mg isoindoline (2.97mmol) are dissolved in 10ml dichloromethane, and the resulting mixture is stirred at room temperature overnight. After addition of water, the mixture was extracted several times with dichloromethane, the combined organic phases were washed, dried over magnesium sulfate and filtered. The solvent was evaporated under reduced pressure. The residue was subjected to column chromatography using dichloromethane to give the title compound.
Example 374B
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
105mg of N- (4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) phenyl) isoindoline-2-carboxamide (0.288mmol) and 53mg of 4-chloro-1, 2-dihydrophthalazin-1-one (0.288mmol) are dissolved in 2.5ml of dioxane. Cesium carbonate (474mg, 1.44mmol) was dissolved in 0.25ml of water, and the resulting solution was added to the reaction mixture. 27.8mg of [1, 1' -bis (diphenylphosphino) -ferrocene ] are added ]After palladium (II) dichloride (0.038mmol), the reaction mixture was purged with nitrogen and stirred in a microwave (Biotage Initiator 2.5) at 110 ℃ for 30 minutes. Removing dioxan under reduced pressureAlkane, water and dichloromethane were added to the residue and the precipitate formed was filtered. After dissolving the solid material in a large amount of methylene chloride/methanol (8: 2), silica gel was added, followed by removal of the solvent under reduced pressure. The residue was purified by column chromatography using 95: 5 dichloromethane/methanol.1H NMR(DMSO-d6，400MHz)：δppm 12.73(s，1H)，8.55(s，1H)，8.33(dd，1H)，7.85-7.92(m，2H)，7.73-7.78(m，3H)，7.48(d，2H)，7.35-7.38(m，2H)，7.30-7.33(m，2H)，4.81(s，4H)。MS(ESI(-))m/e 383.2(M+H)+。
Example 375
N- [4- (isoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 374B, substituting 4-bromoisoquinoline for 4-chloro-1, 2-dihydrophthalazin-1-one. ESI-MS [ M + H + ] ═ 366.1.
Example 376
N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one. ESI-MS [ M + H + ] -382.1.
Example 377
N- [4- (4-oxo-3, 4, 5, 6, 7, 8-hexahydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 377A
2- (4-amino-benzoyl) -cyclohex-1-enecarboxylic acid
To a suspension of 2.2g of magnesium turnings (83.5mmol) in 15mL of tetrahydrofuran was added 0.1mL of 1, 2-dibromoethane to start the Grignard reaction, and then 13.0g of 2- (4-bromophenyl) -1, 1, 1, 3, 3, 3-hexamethyldisilazane (41mmol) in 70mL of tetrahydrofuran was slowly added over 20 minutes at room temperature, followed by further stirring for 30 minutes. The resulting mixture was added dropwise to a solution of 4, 5, 6, 7-tetrahydro-isobenzofuran-1, 3-dione (5.6g) in 70ml of tetrahydrofuran at-78 ℃. The reaction mixture was slowly warmed to room temperature. Sulfuric acid (2ml, 1M) was added and the solvent was removed under reduced pressure. The residue was carefully added to 20mL of 0.5M sulfuric acid solution, and the desired product began to precipitate and was extracted with ethyl acetate. The aqueous phase was acidified and extraction continued with ethyl acetate until pH 4-5 (at least three times). The combined organic phases were washed with brine, dried over magnesium sulfate, filtered and the solvent was evaporated under reduced pressure. Purification of the starting material by column chromatography using 1: 1 ethyl acetate/hexane followed by 100% ethyl acetate yielded the desired product.
Example 377B
4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one
10.3g of 2- (4-amino-benzoyl) -cyclohex-1-enecarboxylic acid (42mmol) are dissolved in 45ml of ethanol, 2.7g (54mmol) of hydrazine hydrate are added and the mixture is heated at reflux for 30 hours. Several hours after heating, the product began to precipitate. After cooling in the refrigerator overnight, the precipitated product was filtered and washed with cold ethanol.
Example 377C
1, 3-dihydro-isoindole-2-carboxylic acid [4- (4-oxo-3, 4, 5, 6, 7, 8-hexahydro-phthalazin-1-yl) -phenyl ] -amide
To a solution of 200mg of 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one (0.829mmol) in 5ml of N, N-dimethylformamide was added 245mg of bis- (2, 5-dioxo-pyrrolidin-1-yl) carbonate (0.912mmol) and the reaction mixture was stirred overnight. 255mg of isoindoline and 0.8ml of N, N-dimethylformamide are added, the precipitate formed is dissolved and the reaction mixture is stirred overnight. Water was added and the precipitate formed was washed with water/methanol and subsequently dried in vacuo to give the crude product. And refluxing the crude product in 20ml of ethanol for 2 hours, cooling to room temperature, filtering and drying to obtain the target product. ESI-MS [ M + H + ] -387.2.
Example 378
N- [4- (8-fluoro-4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C, using 4- (4-amino-phenyl) -5-fluoro-2H-phthalazin-1-one instead of 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one. ESI-MS [ M + H + ] -401.1.
Example 379
5-fluoro-N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-fluoro-2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] -401.1.
Example 380
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-pyrrolidin-1-ylmethyl-2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] -466.2.
Example 381
5- (morpholin-4-ylmethyl) -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-morpholin-4-ylmethyl-2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] -481.3.
Example 382
5-methoxy-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-methoxy-2, 3-dihydro-1H-isoindoline for isoindoline. ESI-MS [ M + H + ] -412.2.
Example 383
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5- (4-methyl-piperazin-1-ylmethyl) -2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] -495.2.
Example 384
5-cyano-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 2, 3-dihydro-1H-isoindole-5-carbonitrile for isoindoline. ESI-MS [ M + H + ] -407.1.
Example 385
5-chloro-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-chloro-2, 3-dihydro-1H-isoindoline for isoindoline. ESI-MS [ M + H + ], 416.1.
Example 386
N- [4- (4-oxo-4, 5-dihydro-3H-2, 3-benzodiazepine-1-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C, using 1- (4-amino-phenyl) -3, 5-dihydro-benzo [ d ]][1，2]Diaza derivatives-4-one instead of 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one. ESI-MS [ M + H +]＝397.2。
Example 387
N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-pyrrolidin-1-ylmethyl-2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] -465.2.
Example 388
N- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) -5-trifluoromethyl-2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one. ESI-MS [ M + H + ] -451.1.
Example 389
5- [ (dimethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and (2, 3-dihydro-1H-isoindol-5-ylmethyl) -dimethyl-amine for isoindoline. ESI-MS [ M + H + ] -439.3.
Example 390
5- [ (diethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and (2, 3-dihydro-1H-isoindol-5-ylmethyl) -diethyl-amine for isoindoline. ESI-MS [ M + H + ] ═ 467.3.
Example 391
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-aminophenyl) isoquinolin-1 (2H) -one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5- (4-methyl-piperazin-1-ylmethyl) -2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] 494.3.
Example 392
5- [ (dimethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and (2, 3-dihydro-1H-isoindol-5-ylmethyl) -dimethyl-amine for isoindoline. ESI-MS [ M + H + ] -440.2.
Example 393
5- [ (diethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and (2, 3-dihydro-1H-isoindol-5-ylmethyl) -diethyl-amine for isoindoline. ESI-MS [ M + H + ] 468.2.
Example 394
N- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -5-trifluoromethyl-2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-pyrrolidin-1-ylmethyl-2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] -534.2.
Example 395
5- [ (1-methylpiperidin-4-yl) oxy ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5- (1-methyl-piperidin-4-yloxy) -2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] 496.2.
Example 396
5- { [ (3R) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5- ((R) -3-fluoro-pyrrolidin-1-ylmethyl) -2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] 484.2.
Example 397
5- { [ (3S) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5- ((S) -3-fluoro-pyrrolidin-1-ylmethyl) -2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] -484.2.
Example 398
5- (azetidin-1-ylmethyl) -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-azetidin-1-ylmethyl-2, 3-dihydro-1H-isoindoline for isoindoline. ESI-MS [ M + H + ], 452.2.
Example 399
N- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 399A
N' - (4-bromobenzoyl) -1H-pyrrole-2-carbohydrazide
To 0.750g of 1H-pyrrole-2-carbohydrazide (5.99mmol) in 50ml of tetrahydrofuran were added 1.315g of 4-bromobenzoyl chloride (5.99mmol) and 1ml of pyridine (11.99mmol) at room temperature under a nitrogen atmosphere. After stirring at room temperature for one hour, the desired product precipitated. Filtration The precipitate was washed with a minimum amount of dichloromethane and methanol and dried to give the title compound.1H NMR(400MHz，DMSO-d6)δ11.63(s，1H)，10.47(s，1H)，10.04(s，1H)，7.84-7.88(m，2H)，7.75(d，J＝8.8，1H)，7.75(q，J＝4.2，1H)，6.91-6.95(m，2H)，6.33-6.15(m，1H)。
Example 399B
2- (4-bromophenyl) -5- (1H-pyrrol-2-yl) -1, 3, 4-oxadiazole
To 1.2g of N' - (4-bromobenzoyl) -1H-pyrrole-2-carbohydrazide (3.89mmol) was added 5ml of phosphorus oxychloride (1.65 mmol). The reaction was stirred at 120 ℃ for 25 minutes. The reaction was cooled to 0 ℃ and ice was added. Filtering the obtained solid, adding water and NH4OH, dichloromethane and ethyl acetate. Purification by chromatography on silica gel (dichloromethane: methanol 9: 1) gives the desired product.1H NMR(400MHz，DMSO-d6)δ12.32(s，1H)，8.05-8.00(m，2H)，7.89-7.83(m，2H)，7.18(td，J＝1.5，2.6，1H)，6.97(ddd，J＝1.5，2.4，3.7，1H)，6.33(dt，J＝2.4，3.6，1H)。13C NMR(400MHz，DMSO-d6)δ110.16，112.49，115.12，122.71，123.96，125.23，128.26，132.49，159.37，161.57。
Example 399C
4- (4-bromophenyl) pyrrolo [1, 2-d ] [1, 2, 4] triazin-1 (2H) -one
To 0.469g of sodium ethoxide (6.89mmol) dissolved in 20ml of ethanol was added 1.0g of 2- (4-bromophenyl) -5- (1H-pyrrol-2-yl) -1, 3, 4-oxadiazole (3.45mmol) at room temperature under a nitrogen atmosphere, and the mixture was stirred at room temperature for 5 minutes. The reaction was heated in a microwave (Biotage Initiator 2.5) at 160 ℃ for 2 hours. The reaction was monitored by TLC (dichloromethane/methanol-9/1). Additional equivalents of sodium ethoxide were added and additional heating was performed until after the reaction was complete (according to TLC). The reaction mixture was concentrated under reduced pressure and adsorbed onto silica gel. The product was purified by silica gel chromatography (gradient: cyclohexane/ethyl acetate 0-100%) to yield The title compound.1H NMR(400MHz，DMSO-d6)δ12.09(s，1H)，7.85-7.78(m，2H)，7.76-7.69(m，2H)，7.39(dd，J＝1.3，2.9，1H)，7.16(dd，J＝1.4，3.8，1H)，6.77(dd，J＝2.9，3.8，1H)。13C NMR(400MHz，DMSO-d6)δ154.22，136.46，131.98，130.90，129.52，124.07，124.00，118.80，114.42，111.01。
Example 399D
4- (4-aminophenyl) pyrrolo [1, 2-d ] [1, 2, 4] triazin-1 (2H) -one
To a solution of 1.181g of 4- (4-bromophenyl) pyrrolo [1, 2-d ] at room temperature under a nitrogen atmosphere][1，2，4]To triazine-1 (2H) -one (4.07mmo1) (in toluene (10ml) were added 0.080g of 2-dicyclohexylphosphino-2' - (N, N-dimethylamino) biphenyl (0.2004mmol), 0.063g of tris (dibenzylideneacetone) dipalladium (0) chloroform adduct (0.061mmol) and 10.58ml of lithium bis (trimethylsilyl) amide (1M in toluene (10.58 mmol)), and the reaction was subsequently heated at 150 ℃ for 5 minutes with a microwave (Biotage Initiator 2.5). Thin layer chromatography (cyclohexane/ethyl acetate 1/1) showed no starting material. After the reaction mixture was cooled, 7ml of 2N hcl aqueous solution was added, the mixture was stirred for 30 minutes, and NaOH aqueous solution (2N) was added to basify the mixture until pH 10. A precipitate formed. The solid was filtered, washed with ether and dried overnight to give the title compound. LCMS: m/z 227.0(M + H). The filtrate was extracted with ethyl acetate. The organic phase was combined with the ether wash and washed with Na2SO4Drying, filtering and evaporating the solvent under reduced pressure. The starting material was adsorbed onto silica (dissolved in ethyl acetate) and then chromatographed on silica gel (cyclohexane: ethyl acetate gradient, product eluted at 80% ethyl acetate) to give additional title compound. 1H NMR(400MHz，DMSO-d6)δ11.85(br.s.，1H)，7.32-7.44(m，3H)，7.09(dd，J＝3.8，1.3Hz，1H)，6.66-6.77(m，3H)，5.67(s，2H)。13C NMR(400MHz，DMSO-d6)δ154.15，150.86，137.98，129.55，123.98，118.70，116.65，113.95，113.32，110.58。
Example 399E
[4- (1-oxo-1, 2-dihydro-pyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) -phenyl ] -carbamic acid phenyl ester
To a suspension of 50mg of 4- (4-aminophenyl) pyrrolo [1, 2-d ] [1, 2, 4] triazin-1 (2H) -one (0.22mmol) in 1ml of tetrahydrofuran at room temperature is added 0.03ml of pyridine (0.3mmol) in 0.5ml of tetrahydrofuran over 5 minutes. Subsequently, 0.03ml of phenyl chloroformate (0.23mmol) dissolved in 3ml of tetrahydrofuran was added over 30 minutes, and the reaction was stirred at room temperature overnight. The solvent was evaporated in vacuo and the mixture was directly bound to silica with dichloromethane. The mixture was purified by silica gel chromatography (4g, cyclohexane: ethyl acetate gradient) to give the crude product, which was purified by column chromatography (cyclohexane: ethyl acetate gradient) to give the title compound.
Example 399F
N- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
40mg of [4- (1-oxo-1, 2-dihydro-pyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) -phenyl ] -carbamic acid phenyl ester (0.115mmol) are dissolved in 0.3ml of DMSO. At room temperature, a mixture of 15mg of isoindoline (0.121mmol) and 0.2ml of DMSO was added, and the reaction was stirred at room temperature overnight. The reaction mixture was diluted in ethyl acetate, washed with water, aqueous HCl, water, aqueous NaOH, and water. The solvent was evaporated under reduced pressure to give the title compound.
Example 400
N- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 400A
5-pyrrolidin-1-ylmethyl-1, 3-dihydro-isoindole-2-carboxylic acid tert-butyl ester
To a solution of 1.25g of tert-butyl 5-hydroxymethyl-1, 3-dihydro-isoindole-2-carboxylate (5.01mmol) in 14ml of dichloromethane was slowly added 0.781ml of methanesulfonyl chloride (10.03mmol) at room temperature. Subsequently, the mixture was heated at reflux for 4 hours. LCMS control showed almost complete formation of the corresponding mesylate, which was not isolated. After cooling to room temperature, 1.244ml pyrrolidine (15.04mmol) was added and the mixture was stirred at room temperature overnight. The reaction was complete according to LCMS. Water was added to the reaction mixture, the acidic aqueous phase was extracted twice with dichloromethane, and the aqueous phase was basified and extracted three times with ethyl acetate. The combined ethyl acetate solution was extracted with brine and extracted with Na2SO4Drying, filtration and removal of the organic solvent under reduced pressure afforded the title compound. The dichloromethane phase was extracted twice with dilute NaOH, once with brine and then with Na2SO4And (5) drying. Filtration and removal of the organic solvent under reduced pressure afforded additional title compound. The two fractions were combined and used in the next step without further purification. LCMS: m/z303.2(M + H).
Example 400B
5-pyrrolidin-1-ylmethyl-2, 3-dihydro-1H-isoindole
To a solution of 1.90g of tert-butyl 5-pyrrolidin-1-ylmethyl-1, 3-dihydro-isoindole-2-carboxylate (starting material; 4.96mmol) in 5ml of dichloromethane was added 3.82ml of trifluoroacetic acid (49.6mmol) and the reaction mixture was stirred at room temperature overnight. Trifluoroacetic acid and dichloromethane were evaporated under reduced pressure, water was added to the residue, the acidic aqueous phase was extracted twice with ethyl acetate, the aqueous phase was basified with dilute NaOH and then extracted three times with dichloromethane. The dichloromethane phase was washed once with brine and Na2SO4Drying, filtering and removing the solvent in vacuum. The title compound was used in the next step without further purification. LCMS: m/z 203.2(M + H).
Example 400C
5-pyrrolidin-1-ylmethyl-1, 3-dihydro-isoindole-2-carboxylic acid [4- (1-oxo-1, 2-dihydro-pyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) -phenyl ] -amide
The title compound was prepared as described in example 399E and example 399F, substituting 5-pyrrolidin-1-ylmethyl-2, 3-dihydro-1H-isoindoline for isoindoline. LCMS: m/z455.2(M + H).
Example 401
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272A using 4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino]Phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester instead of 4-nitro-N-propylbenzamide.1H NMR(400MHz，DMSO-d6)δppm 8.26(s，1H)，7.46-7.48(m，2H)，7.34-7.39(m，2H)，7.28-7.33(m，2H)，7.10-7.13(m，2H)，4.75(s，4H)，4.02-4.08(m，2H)，2.71-2.90(m，2H)，2.57-2.68(m，1H)，1.71-1.76(m，2H)，1.40-1.51(m，2H)，1.42(s，9H)；MS(ESI(-))m/e 420(M-H)-。
Example 402
N- [4- (5-propyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 402A
N- (4-cyanophenyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting 4-isocyanatobenzonitrile for methyl 4-isocyanatobenzoate.
Example 402B
(Z) -N- (4- (N' -carbamimidoyl) phenyl) isoindoline-2-carboxylic acid amide
In a 25mL pressure tube, N- (4-cyanophenyl) isoindoline-2-carboxamide (500mg, 1.899mmol), hydroxylamine hydrochloride (264mg, 3.80mmol) and triethylamine (1.323mL, 9.50mmol) were combined in ethanol (6 mL)/water (0.5 mL). The reaction vessel was sealed and heated at 80 ℃ for four hours. The reaction mixture was diluted with water, the solid was filtered off and washed with water. HPLC purification provided the title compound.
Example 402C
N- [4- (5-propyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
In a 4mL vial, (Z) -N- (4- (N' -hydroxycarbamimidoyl) phenyl) isoindoline-2-carboxamide (50mg, 0.169mmol), butyric acid (0.017mL, 0.186mmol), 1-hydroxybenzotriazole hydrate (12.92mg, 0.084mmol), and N-methylmorpholine (0.056mL, 0.506mmol) were combined in anhydrous dimethylformamide (2 mL). To this solution was added N- (3-dimethylaminopropyl) -N' -ethylcarbodiimide hydrochloride (48.5mg, 0.253mmol) and the mixture was stirred at ambient temperature overnight. The solution was diluted with ethyl acetate, washed with water, saturated aqueous sodium bicarbonate and brine. The organic layer was dried over sodium sulfate, decanted, and concentrated. The residue was taken up in anhydrous toluene (1ml) and the mixture was heated at 110 ℃ for 2 days. Diluting the reaction with water; and the solid formed was filtered and washed with water and ether to provide the title compound. 1H NMR(500MHz，DMSO-d6)δppm 8.68(s，1H)，7.89-7.91(m，2H)，7.78-7.80(m，2H)，7.36-7.40(m，2H)，7.30-7.34(m，2H)，4.76-4.85(m，4H)，2.96(t，J＝7.4Hz，2H)，1.81(hex，J＝7.4Hz，2H)，0.99(t，J＝7.4Hz，3H)；MS(ESI(-))m/e347(M-H)-。
Example 403
N- [4- (piperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 2D using 4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino]Phenyl } piperidine-1-carboxylic acid tert-butyl ester instead of tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.1HNMR(500MHz，DMSO-d6)δppm 8.28(s，1H)，7.46-7.48(m，2H)，7.34-7.37(m，2H)，7.30-7.33(m，2H)，7.09-7.12(m，2H)，4.75-4.76(bs，4H)，3.09-3.17(m，2H)，2.68(td，J＝12.3，2.6Hz，2H)，2.57(tt，J＝12.0，3.4Hz，1H)，1.71-1.75(m，2H)，1.56(qd，J＝12.5，3.9Hz，2H)；MS(ESI(+))m/e 322(M+H)+。
Example 404
N- {5- [ ((3R) -tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxamide and N- {5- [ ((3S) -tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxamide
The title compound was prepared as described in example 1C, substituting (tetrahydrofuran-3-yl) methylamine for 3-phenylpropan-1-amine and 6- (isoindoline-2-carboxamido) nicotinic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm 9.26(s，1H)，8.74(d，J＝2.4Hz，1H)，8.56-8.60(m，1H)，8.14(dd，J＝8.8，2.5Hz，1H)，8.00(d，J＝8.8Hz，1H)，7.26-7.40(m，4H)，4.59-5.02(m，4H)，3.75(td，J＝8.0，5.7Hz，1H)，3.69(dd，J＝8.5，6.9Hz，1H)，3.59-3.66(m，1H)，3.48(dd，J＝8.5，5.2Hz，1H)，3.18-3.31(m，2H)，2.43-2.51(m，1H)，1.90-1.99(m，1H)，1.56-1.65(m，1H)；MS(ESI(-))m/e365(M-H)-。
Example 405
N- [4- (1-butyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting butyryl chloride for acetyl chloride, N- [4- (piperidin-4-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(400MHz，DMSO-d6)δppm 8.27(s，1H)，7.46-7.49(m，2H)，7.34-7.39(m，2H)，7.28-7.33(m，2H)，7.11-7.14(m，2H)，4.75-4.76(bs，4H)，4.52-4.57(m，1H)，3.94-4.00(m，1H)，3.03-3.11(m，1H)，2.64-2.75(m，1H)，2.51-2.63(m，1H)，2.31(t，J＝7.4Hz，2H)，1.73-1.81(m，2H)，1.47-1.59(m，3H)，1.32-1.47(m，1H)，0.85-0.95(m，3H)；MS(ESI(+))m/e392(M+H)+。
Example 406
N- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting isobutyryl chloride for acetyl chloride, N- [4- (piperidin-4-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(500MHz，DMSO-d6)δppm 8.28(s，1H)，7.46-7.48(m，2H)，7.34-7.39(m，2H)，7.29-7.33(m，2H)，7.12-7.14(m，2H)，4.75-4.76(bs，4H)，4.53-4.58(m，1H)，4.03-4.07(m，1H)，3.06-3.14(m，1H)，2.86-2.93(m，1H)，2.67-2.74(m，1H)，2.53-2.61(m，1H)，1.75-1.84(m，2H)，1.45-1.56(m，1H)，1.33-1.45(m，1H)，1.03(d，J＝6.7Hz，3H)，1.00(d，J＝6.6Hz，3H)；MS(ESI(-))m/e 390(M-H)-。
Example 407
N- [4- (1-benzoylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride, N- [4- (piperidin-4-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(500MHz，DMSO-d6)δppm 8.29(s，1H)，7.47-7.50(m，2H)，7.41-7.47(m，5H)，7.34-7.38(m，2H)，7.29-7.33(m，2H)，7.16-7.18(m，2H)，4.75-4.76(bs，4H)，4.54-4.64(m，1H)，3.57-3.74(m，1H)，3.02-3.21(m，1H)，2.79-2.93(m，1H)，2.75(tt，J＝11.9，3.4Hz，1H)，1.68-1.88(m，2H)，1.54-1.63(m，2H)；MS(ESI(-))m/e 424(M-H)-。
Example 408
N- {4- [5- (3-methylbutyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 402C, substituting 4-methylvaleric acid for butyric acid.1H NMR(500MHz，DMSO-d6)δppm 8.69(s，1H)，7.89-7.91(m，2H)，7.77-7.79(m，2H)，7.36-7.39(m，2H)，7.31-7.34(m，2H)，4.80-4.81(bs，4H)，2.96-3.00(m，2H)，1.66-1.72(m，2H)，1.59-1.67(m，1H)，0.93(d，J＝6.4Hz，6H)；MS(ESI(-))m/e 375(M-H)-。
Example 409
N- [4- (5-benzyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 402C, substituting phenylacetic acid for butyric acid.1H NMR(500MHz，DMSO-d6)δppm 8.69(s，1H)，7.87-7.90(m，2H)，7.77-7.79(m，2H)，7.35-7.42(m，6H)，7.29-7.34(m，3H)，4.75-4.84(m，4H)，4.42(s，2H)；MS(ESI(+))m/e 397(M+H)+。
Example 410
N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Reacting N- (4- { [ tetrahydrofuran-3-ylmethyl)]Carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide (250mg) racemic mixture was dissolved in methanol and separated using SCF-LC (ChiralPak AD-H21X 250mm column) to provide N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl]Carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide.1HNMR(300MHz，DMSO-d6)δppm 8.58(s，1H)，8.38(t，J＝5.7Hz，1H)，7.75-7.79(m，2H)，7.64-7.69(m，2H)，7.30-7.41(m，4H)，4.78-4.79(bs，4H)，3.57-3.78(m，3H)，3.48(dd，J＝8.5，5.2Hz，1H)，3.17-3.28(m，2H)，2.41-2.50(m，1H)，1.87-2.04(m，1H)，1.54-1.66(m，1H)；MS(ESI(+))m/e 366(M+H)+。
Example 411
N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Reacting N- (4- { [ tetrahydrofuran-3-ylmethyl)]Carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide (250mg) racemic mixture was dissolved in methanol and separated using SCF-LC (ChiralPak AD-H21X 250mm column) to provide N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl]Carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide.1HNMR(300MHz，DMSO-d6)δppm 8.57(s，1H)，8.38(t，J＝5.7Hz，1H)，7.75-7.79(m，2H)，7.64-7.69(m，2H)，7.30-7.39(m，4H)，4.78-4.79(bs，4H)，3.57-3.78(m，3H)，3.48(dd，J＝8.5，5.3Hz，1H)，3.13-3.29(m，2H)，2.40-2.50(m，1H)，1.87-2.07(m，1H)，1.54-1.66(m，1H)；MS(ESI(+))m/e 366(M+H)+。
Example 422
4- {6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] -1H-benzimidazol-2-yl } piperazine-1-carboxylic acid tert-butyl ester
Example 422A
4- (5-Nitro-1H-benzo [ d ] imidazol-2-yl) piperazine-1-carboxylic acid tert-butyl ester
In a 20mL sealed tube, a mixture of piperazine-1-carboxylic acid tert-butyl ester (0.943g, 5.06mmol), 2-chloro-5-nitro-1H-benzo [ d ] imidazole (0.5g, 2.53mmol), and ethanol (9.5mL) was heated at 135 ℃ for 2 hours under a nitrogen atmosphere. The reaction was concentrated and the residue was purified by reverse phase chromatography to afford the title compound.
Example 422B
4- (5-amino-1H-benzo [ d ] imidazol-2-yl) piperazine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 274, substituting 4- (5-nitro-1H-benzo [ d ] imidazol-2-yl) piperazine-1-carboxylic acid tert-butyl ester for 5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide.
Example 422C
4- {6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] -1H-benzimidazol-2-yl } piperazine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272B using 4- (5-amino-1H-benzo [ d ]]Imidazol-2-yl) piperazine-1-carboxylic acid tert-butyl ester instead of 4-amino-N-propylbenzamide, isoindoline instead of isoindoline-5-carboxylic acid methyl ester hydrochloride.1H NMR(400MHz，DMSO-d6Temperature 90 ℃ delta ppm 10.90-11.08(bs, 1H), 7.84-7.85(m, 1H), 7.46-7.48(m, 1H), 7.27-7.35(m, 4H), 7.04-7.06(m, 2H), 4.76(s, 4H), 3.46(s, 8H), 1.44(s, 9H); MS (ESI (+)) M/e 463(M + H)+。
Example 423
N- [2- (piperazin-1-yl) -1H-benzimidazol-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 2D using 4- {6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino]-1H-benzimidazol-2-yl } piperazine-1-carboxylic acid tert-butyl ester instead of 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamic acid tert-butyl ester. 1H NMR(300MHz，DMSO-d6)δppm 11.04-11.29(m，1H)，8.08-8.12(bs，1H)，7.41-7.58(m，1H)，7.24-7.39(m，4H)，7.04-7.06(m，2H)，4.76(s，4H)，3.37-3.44(m，4H)，2.85-2.89(m，4H)；MS(ESI(+))m/e363(M+H)+。
Example 424
N- [4- (propylcarbamoyl) phenyl ] -5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
In a sealed vial, potassium vinyltrifluoroborate (100mg, 0.75mmol), 5-bromo-N- (4- (propylcarbamoyl) phenyl) isohydrogenA mixture of indole-2-carboxamide (150mg, 0.37mmol), bis (triphenylphosphine) palladium (II) chloride and saturated aqueous sodium bicarbonate solution (0.62ml) in dimethylformamide was heated at 85 ℃ for 5 h. The reaction was poured into water, filtered, dried and purified by reverse phase chromatography to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 8.57(s，1H)，8.25(t，J＝5.7Hz，1H)，7.75-7.78(m，2H)，7.63-7.67(m，2H)，7.47(s，1H)，7.42(dd，J＝7.9，1.5Hz，1H)，7.34(d，J＝7.8Hz，1H)，6.77(dd，J＝17.6，10.9Hz，1H)，5.85(dd，J＝17.6，1.0Hz，1H)，5.27(d，J＝11.0Hz，1H)，4.77-4.78(bs，4H)，3.16-3.22(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 350(M+H)+。
Example 428
N- {4- [5- (tetrahydrofuran-3-yl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 402C, substituting tetrahydrofuran-3-carboxylic acid for butyric acid.1H NMR(500MHz，DMSO-d6)δppm 8.69(s，1H)，7.89-7.92(m，2H)，7.78-7.81(m，2H)，7.36-7.40(m，2H)，7.30-7.34(m，2H)，4.80-4.81(bs，4H)，4.08(dd，J＝8.6，7.6Hz，1H)，3.97(dd，J＝8.6，5.4Hz，1H)，3.86-3.95(m，2H)，3.79-3.85(m，1H)，2.40(dddd，J＝12.5，9.0，7.6，5.9Hz，1H)，2.26(ddt，J＝7.7，12.4，6.2Hz，1H)；MS(ESI(-))m/e375(M-H)-。
Example 429
N- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
In 4ml, N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide (50mg, 0.157mmol) and isobutyraldehyde (0.014ml, 0.157mmol) were mixed in anhydrous dichloroethane (2ml) at room temperature. Sodium triacetoxyborohydride (46.4mg, 0.219mmol) was added and the reaction was stirred overnight. Reacting the mixture The mixture was diluted with water, ethyl acetate and saturated aqueous sodium bicarbonate. The layers were separated and the organic layer was washed with brine. The organic layer was diluted with methanol, dried over sodium sulfate, filtered and concentrated. The residue was purified by flash chromatography to afford the title compound.1H NMR(400MHz，DMSO-d6)δppm 8.35(s，1H)，7.53-7.55(m，2H)，7.30-7.38(m，6H)，6.06-6.08(m，1H)，4.77(s，4H)，3.01-3.03(m，2H)，2.57(t，J＝5.6Hz，2H)，2.41-2.47(m，2H)，2.14(d，J＝7.3Hz，2H)，1.77-1.88(m，1H)，0.88(d，J＝6.5Hz，6H)；MS(ESI(-))m/e 374(M-H)-。
Example 432
N- {4- [1- (4-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting 4-methylbenzoyl chloride for acetyl chloride and N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1HNMR(400MHz，DMSO-d6)δppm 8.38(s，1H)，7.55-7.58(m，2H)，7.20-7.39(m，10H)，6.01-6.21(m，1H)，4.77(s，4H)，3.93-4.36(m，2H)，3.43-3.90(m，2H)，2.48-2.57(m，2H)，2.36(s，3H)；MS(ESI(+))m/e438(M+H)+。
Example 433
N- [4- (1-benzyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 429 with benzaldehyde replacing isobutyraldehyde.1H NMR(400MHz，DMSO-d6)δppm 8.36(s，1H)，7.52-7.55(m，2H)，7.20-7.42(m，11H)，6.06-6.08(m，1H)，4.76-4.77(bs，4H)，3.58(s，2H)，3.04-3.06(m，2H)，2.63(t，J＝5.6Hz，2H)，2.42-2.49(m，2H)；MS(ESI(+))m/e 410(M+H)+。
Example 440
N- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-3-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting pyridin-3-ylboronic acid for 1H-pyrazol-3-ylboronic acid, 5-bromo-N- [4- (propylcarbamoyl) phenyl ]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxylic acid amide.1H NMR(300MHz，DMSO-d6)δppm 8.91(dd，J＝2.4，0.9Hz，1H)，8.63(s，1H)，8.58(dd，J＝4.7，1.6Hz，1H)，8.27(t，J＝5.6Hz，1H)，8.10(ddd，J＝7.9，2.4，1.6Hz，1H)，7.73-7.79(m，3H)，7.65-7.70(m，3H)，7.48-7.53(m，2H)，4.79-4.91(m，4H)，3.15-3.23(m，2H)，1.54(s，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 401(M+H)+。
Example 441
N- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-4-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting pyridin-4-ylboronic acid for 1H-pyrazol-3-ylboronic acid, 5-bromo-N- [4- (propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxylic acid amide.1H NMR(300MHz，DMSO-d6)δppm 8.62-8.66(m，3H)，8.25(t，J＝5.6Hz，1H)，7.70-7.81(m，6H)，7.64-7.69(m，2H)，7.52(d，J＝8.0Hz，1H)，4.85-4.92(m，4H)，3.16-3.22(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)。MS(ESI(+))m/e 401(M+H)+。
Example 442
N5- (2-methoxyethyl) -N2- {4- [ (propylamino) carbonyl group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide
The title compound was prepared as described in example 1C, using 2-methoxyethylamineSubstituted 3-phenylpropan-1-amine, 2- { [4- (propylcarbamoyl) phenyl]Carbamoyl } isoindoline-5-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.61(s，1H)，8.54(d，J＝5.3Hz，1H)，8.26(t，J＝5.7Hz，1H)，7.79-7.85(m，2H)，7.73-7.80(m，2H)，7.63-7.67(m，2H)，7.45(d，J＝7.8Hz，1H)，4.81-4.83(bs，4H)，3.39-3.51(m，4H)，3.27(s，3H)，3.03-3.22(m，2H)，1.46-1.59(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 425(M+H)+。
Example 443
N- (4-cyanophenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting 4-isocyanatobenzonitrile for methyl 4-isocyanatobenzoate.1H NMR(400MHz，DMSO-d6)δppm 8.83(s，1H)，7.78-7.82(m，2H)，7.69-7.73(m，2H)，7.31-7.39(m，4H)，4.79-4.81(bs，4H)；MS(ESI(+))m/e 264(M+H)+。
Example 444
N- [4- (trifluoromethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting 1-isocyanato-4- (trifluoromethyl) benzene for methyl 4-isocyanatobenzoate.1H NMR(400MHz，DMSO-d6)δppm8.74(s，1H)，7.80-7.83(m，2H)，7.60-7.63(m，2H)，7.30-7.39(m，4H)，4.79-4.80(bs，4H)；MS(ESI(+))m/e 307(M+H)+。
Example 450
5- (1, 2-dihydroxyethyl) -N- {4- [ (propylamino) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Reacting N- [4- (propylcarbamoyl) phenyl]Suspension of 5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide (0.03g, 0.086mmol) in tetrahydrofuran (1ml) and 2-propanol (0.3ml)The suspension was treated with osmium tetroxide (2.5% wt.% solution in 2-methyl-2-propanol) (0.108ml, 8.59. mu. mol). The reaction mixture was treated with N-methylmorpholine-N-oxide (0.030g, 0.258 mmol). The reaction mixture was stirred at room temperature overnight, quenched with aqueous sodium sulfite solution, and extracted with ethyl acetate. The combined organic layers were washed with brine, dried over anhydrous sodium sulfate and concentrated in vacuo. Flash chromatography was performed to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 8.55(s，1H)，8.25(t，J＝5.7Hz，1H)，7.74-7.78(m，2H)，7.63-7.68(m，2H)，7.27-7.33(m，3H)，5.24(d，J＝4.2Hz，1H)，4.75-4.77(bs，4H)，4.70(t，J＝5.8Hz，1H)，4.53-4.59(m，1H)，3.43(t，J＝5.8Hz，2H)，3.16-3.23(m，2H)，1.42-1.63(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 384(M+H)+。
Example 451
N- [4- (1-benzoylpiperidin-4-yl) butyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 451A
4- (4- (5-Cyanoisoindoline-2-carboxamido) butyl) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272B using tert-butyl 4- (4-aminobutyl) piperidine-1-carboxylate instead of 4-amino-N-propylbenzamide and isoindoline-5-carbonitrile instead of methyl isoindoline-5-carboxylate hydrochloride.
Example 451B
5-cyano-N- (4- (piperidin-4-yl) butyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D, substituting 4- (4- (5-cyanoisoindoline-2-carboxamido) butyl) piperidine-1-carboxylic acid tert-butyl ester for 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate tert-butyl ester.
Example 451C
N- [4- (1-benzoylpiperidin-4-yl) butyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride and 5-cyano-N- (4- (piperidin-4-yl) butyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 7.83(s，1H)，7.75(dd，J＝7.9，1.5Hz，1H)，7.53(d，J＝7.9Hz，1H)，7.41-7.44(m，3H)，7.31-7.38(m，2H)，6.36(t，J＝5.5Hz，1H)，4.60-4.64(m，4H)，4.30-4.53(m，1H)，3.42-3.71(m，1H)，3.02-3.10(m，2H)，2.64-3.00(m，2H)，1.56-1.84(m，2H)，1.37-1.54(m，3H)，1.24-1.31(m，4H)，0.93-1.16(m，2H)；MS(ESI(+))m/e431(M+H)+。
Example 452
N- (1 '-butyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 452A
N- (5-bromopydin-2-yl) isoindoline-2-carboxamide
The title compound was prepared as described in example 344A, substituting 5-bromopiridine-2-amine for tert-butyl 5-aminoisoindoline-2-carboxylate.
Example 452B
4- (6- (isoindoline-2-carboxamido) pyridin-3-yl) -5, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester
The title compound was prepared as described in example 280, using tert-butyl 4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylate instead of 1H-pyrazol-3-ylboronic acid and N- (5-bromopiridin-2-yl) isoindoline-2-carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.
Example 452C
N- (5- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-2-yl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D, substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (6- (isoindoline-2-carboxamido) pyridin-3-yl) -5, 6-dihydropyridine-1 (2H) -carboxylate.
Example 452D
N- (1 '-butyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting butyryl chloride for acetyl chloride and N- (5- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-2-yl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(500MHz，DMSO-d6)δppm 8.92-8.95(bs，1H)，8.32-8.35(m，1H)，7.64-7.97(m，2H)，6.94-7.38(m，4H)，6.16-6.22(bs，1H)，4.45-5.02(m，4H)，4.08-4.15(m，2H)，3.62-3.68(m，2H)，2.23-2.65(m，4H)，1.46-1.64(m，2H)，0.87-0.93(m，3H)；MS(ESI(+))m/e 391(M+H)+。
Table 6.
The title compound was prepared as described in example 1C, substituting N- (5- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-2-yl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 455
N- [2- (4-acetylpiperazin-1-yl) -1H-benzimidazol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, using N- [2- (piperazin-1-yl) -1H-benzimidazol-6-yl]1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(500MHz，DMSO-d6Temperature 90 ℃ delta ppm 11.01-11.10(bs, 1H), 7.89-7.91(bs, 1H), 7.44-7.52(m, 1H), 7.32-7.35(m, 2H), 7.27-7.31(m, 2H), 7.03-7.06(m, 2H), 4.76(s, 4H), 3.55-3.62(m, 4H), 3.46-3.51(m, 4H), 2.04(s, 3H); MS (ESI (+)) M/e 405(M + H)+。
Table 7.
The following examples were prepared essentially as described in example 1C, substituting the appropriate tetrahydropyridine for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 495
N- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (5- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-2-yl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and benzoic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ ppm 8.51(bs, 1H), 8.32(d, J ═ 2.5Hz, 1H), 7.90(d, J ═ 8.7Hz, 1H), 7.77(dd, J ═ 8.7, 2.5Hz, 1H), 7.48-7.39(m, 5H), 7.36-7.25(m, 4H), 6.16(bs, 1H), 4.81(s, 4H), 4.18(m, 2H), 3.68(m, 2H), 2.55(m, 2H); MS (ESI (+)) M/e 425(M + H)+。
Example 496
N- (4- { [6- (benzoylamino) hexyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride forAcetyl chloride, N- {4- [ (6-aminohexyl) carbamoyl]Phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxylic acid amide.1HNMR(300MHz，DMSO-d6)δppm 8.57(s，1H)，8.43(t，J＝5.6Hz，1H)，8.25(t，J＝5.6Hz，1H)，7.81-7.86(m，2H)，7.74-7.78(m，2H)，7.63-7.67(m，2H)，7.41-7.54(m，3H)，7.29-7.39(m，4H)，4.78-4.79(bs，4H)，3.15-3.27(m，4H)，1.44-1.64(m，4H)，1.19-1.39(m，4H)；MS(ESI(+))m/e485(M+H)+。
Embodiment 497
N- [4- ({4- [ (benzoylamino) methyl ] benzyl } carbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride, N- (4- { [4- (aminomethyl) benzyl ]Carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxylic acid amide.1H NMR(300MHz，DMSO-d6)δppm 9.01(t，J＝6.0Hz，1H)，8.83(t，J＝5.9Hz，1H)，8.60(s，1H)，7.85-7.91(m，2H)，7.78-7.83(m，2H)，7.63-7.68(m，2H)，7.36-7.56(m，4H)，7.27(s，4H)，7.21-7.26(m，1H)，7.10-7.19(m，1H)，4.72-4.81(m，4H)，4.40-4.48(m，4H)；MS(ESI(+))m/e523(M+H)+。
Table 8.
The following examples were prepared essentially as in example 1C, substituting N- (4- (piperazin-1-yl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 542
5-cyano-N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A substituting 4-phenylbutyl isocyanate for methyl 4-isocyanatobenzoate and 5-cyanoisoindoline for isoindoline.1HNMR(300MHz，DMSO-d6)δppm 7.82(s，1H)，7.74(dd，J＝7.9，1.5Hz，1H)，7.53(d，J＝7.9Hz，1H)，7.24-7.31(m，2H)，7.08-7.22(m，3H)，6.38(t，J＝5.6Hz，1H)，4.59-4.64(m，4H)，3.06-3.13(m，2H)，2.58(t，J＝7.5Hz，2H)，1.53-1.68(m，2H)，1.36-1.51(m，2H)；MS(ESI(+))m/e319(M+H)+。
Example 543
N- [4- (1-butanoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 543A
N- (4-bromophenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 1A substituting 4-bromophenyl isocyanate for methyl 4-isocyanatobenzoate and 2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine for isoindoline.
Example 543B
4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) -5, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester
The title compound was prepared as described in example 280, substituting 4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester for 1H-pyrazol-3-ylboronic acid and N- (4-bromophenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.
Example 543C
N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 2D, substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) -5, 6-dihydropyridine-1 (2H) -carboxylate.
Example 543D
N- [4- (1-butanoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 278, substituting butyryl chloride for acetyl chloride, N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c)]Pyridine-2 (3H) -carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1HNMR(400MHz，DMSO-d6)δppm 8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.46(s，1H)，7.54-7.57(m，2H)，7.43(d，J＝5.0Hz，1H)，7.32-7.39(m，2H)，6.09-6.11(m，1H)，4.79-4.82(m，4H)，4.08-4.14(m，2H)，3.58-3.68(m，2H)，2.39-2.55(m，2H)，2.34(dt，J＝19.9，7.4Hz，2H)，1.47-1.62(m，2H)，0.88-0.93(m，3H)；MS(ESI(+))m/e 391(M+H)+。
Example 544
N- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 278, substituting isobutyryl chloride for acetyl chloride, N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c ]]Pyridine-2 (3H) -carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1HNMR(400MHz，DMSO-d6)δppm 8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.46(s，1H)，7.54-7.57(m，2H)，7.43(d，J＝5.1Hz，1H)，7.34-7.38(m，2H)，6.10-6.13(bs，1H)，4.79-4.82(m，4H)，4.07-4.21(m，2H)，3.67-3.70(m，2H)，2.85-3.01(m，1H)，2.39-2.55(m，2H)，0.97-1.08(m，6H)；MS(ESI(+))m/e 391(M+H)+。
Example 545
N- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride, N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c)]Pyridine-2 (3H) -carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1HNMR(400MHz，DMSO-d6)δppm 8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.46(s，1H)，7.55-7.58(m，2H)，7.42-7.49(m，6H)，7.35-7.41(m，2H)，5.98-6.21(m，1H)，4.79-4.82(m，4H)，3.95-4.39(m，2H)，3.79-3.93(m，1H)，3.51-3.61(m，1H)，2.46-2.60(m，2H)；MS(ESI(+))m/e425(M+H)+
Table 9.
The following example was prepared essentially as in example 1C, substituting N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-C ] pyridine-2 (3H) -carboxamide for 3-phenylpropan-1-amine and the corresponding carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 547
N- [4- (1-oxo-2, 3-dihydro-1H-isoindol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-phenyl) -2, 3-dihydro-isoindol-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one. ESI-MS [ M + H + 370.1.
Example 548
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 377C, substituting 2, 3-dihydro-1H-pyrrolo [3, 4-C ] pyridine for isoindoline. ESI-MS [ M + H + ] -384.1.
Example 549
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide
The title compound was prepared as described in example 377C, substituting 6, 7-dihydro-5H-pyrrolo [3, 4-b ] pyridine for isoindoline. ESI-MS [ M + H + ] 384.1.
Example 550
N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-cyclohex-1-enyl) -2H-isoquinolin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one. ESI-MS [ M + H + ] 386.2.
Example 551
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-cyclohex-1-enyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one. ESI-MS [ M + H + ] 387.2.
Example 552
N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 377C substituting 4- (4-amino-cyclohex-1-enyl) -2H-phthalazin-1-one for 4- (4-aminophenyl) -5, 6, 7, 8-tetrahydro-2H-phthalazin-1-one and 5-pyrrolidin-1-ylmethyl-2, 3-dihydro-1H-isoindole for isoindoline. ESI-MS [ M + H + ] 470.2.
Example 557
N- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 1-isopentyl-1H-pyrazol-4-amine dihydrochloride for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride in example 272B.1H NMR(300MHz，DMSO-d6)δppm 8.39(s，1H)，7.74(s，1H)，7.39(s，1H)，7.38-7.26(m，4H)，4.69(s，4H)，4.04(t，J＝7.1Hz，2H)，1.81-1.57(m，2H)，1.52-1.37(m，1H)，0.89(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 299(M+H)+。
Example 558
N- [1- (2-phenylethyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 1-phenylethyl-1H-pyrazol-4-amine dihydrochloride for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride in example 272B.1H NMR(300MHz，DMSO-d6)δppm 8.39(s，1H)，7.68(s，1H)，7.42(s，1H)，7.39-7.23(m，6H)，7.24-7.15(m，3H)，4.68(bs，4H)，4.27(t，J＝7.3Hz，2H)，3.07(t，J＝7.3Hz，2H)；MS(ESI(+))m/e 333(M+H)+。
Example 559
N5- [2- (dimethylamino) ethyl group]-N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide
The title compound was prepared as described in example 1C substituting N1, N1-dimethylethane-1, 2-diamine for 3-phenylpropan-1-amine, 2- { [4- (propylcarbamoyl) phenyl]Carbamoyl } isoindoline-5-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1HNMR(300MHz，DMSO-d6)δppm 9.28(s，1H)，8.70(t，J＝5.6Hz，1H)，8.62(s，1H)，8.26(t，J＝5.6Hz，1H)，7.86-7.74(m，4H)，7.68-7.61(m，2H)，7.49(d，J＝7.8Hz，1H)，4.84(bs，4H)，3.66-3.55(m，2H)，3.29-3.12(m，4H)，2.90-2.80(m，6H)，2.28-1.46(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 438(M+H)+。
Example 560
5- (morpholin-4-ylcarbonyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting morpholine for 3-phenylpropan-1-amine, 2- { [4- (propylcarbamoyl) phenyl [ ]]Carbamoyl } isoindoline-5-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.61(s，1H)，8.26(t，J＝5.7Hz，1H)，7.80-7.73(m，2H)，7.69-7.62(m，2H)，7.47-7.41(m，2H)，7.35(dd，J＝7.7，1.6Hz，1H)，4.82(bs，4H)，3.73-3.43(m，6H)，3.28-3.12(m，4H)，1.60-1.44(m，2H)，0.89(t，J＝7.4Hz，3H)；MS(ESI(+))m/e 437(M+H)+。
Example 561
N- (4- { benzyl [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N-benzyl-3-morpholinopropan-1-amine for 3-phenylpropan-1-amine. 1H NMR(400MHz，DMSO-d6Delta ppm at 90 ℃ 8.28(s, 1H), 7.65-7.59(m, 2H), 7.39-7.25(m, 11H), 4.79(bs, 4H), 4.63(s, 2H), 3.52-3.45(m, 4H), 3.35-3.27(m, 2H), 2.27-2.20(m, 4H), 2.17(t, 2H), 1.69-1.60(m, 2H); MS (ESI (+)) M/e 499(M + H)+。
Example 563
5-bromo-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 563A
2-cyclopentyl-N- (4-nitrophenyl) acetamide
The title compound was prepared as described in example 278, substituting 2-cyclopentylacetyl chloride for acetyl chloride and 4-nitroaniline for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.
Example 563B
N- (4-aminophenyl) -2-cyclopentyl acetamide
The title compound was prepared as described in example 274 substituting 2-cyclopentyl-N- (4-nitrophenyl) acetamide for 5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide.
Example 563C
5-bromo-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting N- (4-aminophenyl) -2-cyclopentyl acetamide for 4-amino-N-propylbenzamide and 5-bromoisoindoline for methyl isoindoline-5-carboxylate hydrochloride. 1H NMR(300MHz，DMSO-d6)δppm9.68(s，1H)，8.29(s，1H)，7.65-7.55(m，1H)，7.53-7.36(m，5H)，7.36-7.26(m，1H)，4.79-4.65(m，4H)，2.33-2.16(m，3H)，1.85-1.68(m，2H)，1.68-1.41(m，4H)，1.29-1.09(m，2H)；MS(ESI(+))m/e442(M+H)+。
Example 565
4- { [ (5-cyano-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoic acid methyl ester
The title compound was prepared as described in example 1A, substituting 5-cyanoisoindoline for isoindoline.1H NMR(300MHz，DMSO-d6)δppm 8.81(s，1H)，7.91-7.82(m，3H)，7.82-7.77(m，1H)，7.76-7.69(m，2H)，7.59(d，J＝7.9Hz，1H)，4.89-4.81(m，4H)，3.81(s，3H)；MS(ESI(+))m/e 322(M+H)+.
Example 566
N- (4- { (E) - [ (benzyloxy) imino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 566A
N- (4-formylphenyl) isoindoline-2-carboxamide
The title compound was prepared as described in example 272B substituting 4-aminobenzaldehyde for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.
Example 566B
N- (4- { (E) - [ (benzyloxy) imino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
In an 8mL sealed vial, N- (4-formylphenyl) isoindoline-2-carboxamide (50mg, 0.188mmol) was combined with methanol (1 mL). O-benzylhydroxylamine hydrochloride (45.0 mg) was then added，0.282mmol) and sodium acetate (46.0mg, 0.338mmol) in water (1.000ml) and the reaction was stirred at room temperature overnight. The reaction was diluted with water and the product was extracted with dichloromethane. The organic layer was washed with brine, dried over sodium sulfate, decanted, and concentrated. Chromatographic purification provided the title compound. 1H NMR (400MHz, DMSO-d) 6)δppm 8.55(s，1H)，8.21(s，1H)，7.65(m，2H)，7.50(m，2H)，7.44-7.28(m，9H)，5.14(s，2H)，4.78(bs，4H)；MS(ESI(+))m/e 372(M+H)+。
Example 573
N- [4- (3-Aminopyrrolidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 339D.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ ppm 7.76(bs, 1H), 7.36-7.31(m, 2H), 7.31-7.25(m, 4H), 6.46-6.42(m, 2H), 4.73(bs, 4H), 3.56(p, J ═ 5.8Hz, 1H), 3.41-3.36(m, 1H), 3.35-3.28(m, 1H), 3.24-3.15(m, 3H), 2.85(dd, J ═ 9.1, 4.9Hz, 1H), 2.13-2.05(m, 1H), 1.73-1.64(m, 1H); MS (ESI (+)) M/e 323(M + H)+。
Example 574
N- {6- [ (3-methylbutyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 574A
5- (isoindoline-2-carboxamido) picolinic acid methyl ester
The title compound was prepared as described in example 272B substituting methyl 5-aminopyridinecarboxylate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.
Example 574B
5- (isoindoline-2-carboxamido) picolinic acid
The title compound was prepared as described in example 1B substituting 5- (isoindoline-2-carboxamido) picolinic acid methyl ester for 4- (isoindoline-2-carboxamido) benzoic acid methyl ester.
Example 574C
N- {6- [ (3-methylbutyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 5- (isoindoline-2-carboxamido) picolinic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm 8.85(m，2H)，8.57(t，J＝6.1Hz，1H)，8.17(dd，J＝8.5，2.4Hz，1H)，7.94(d，J＝8.5Hz，1H)，7.41-7.29(m，4H)，4.79(m，4H)，3.35(m，2H)，1.59(m，1H)，1.42(q，J＝7.1Hz，2H)，0.90(d，J＝6.6Hz，6H)；MS(ESI(+))m/e353(M+H)+。
Example 575
N- {6- [ (3-phenylpropyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 5- (isoindoline-2-carboxamido) picolinic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm 8.86(m，2H)，8.68(t，J＝6.0Hz，1H)，8.18(dd，J＝8.6，2.5Hz，1H)，7.95(d，J＝8.5Hz，1H)，7.41-7.14(m，9H)，4.81(bs，4H)，3.35(m，2H)，2.61(t，J＝7.6Hz，2H)，1.84(m，2H)；MS(ESI(+))m/e 401(M+H)+.
Example 576
N- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting (tetrahydrofuran-3-yl) methylamine for 3-phenylpropan-1-amine and 5- (isoindoline-2-carboxamido) picolinic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm8.87(m，2H)，8.78(t，J＝6.1Hz，1H)，8.18(dd，J＝8.5，2.5Hz，1H)，7.95(d，J＝8.5Hz，1H)，7.42-7.26(m，4H)，4.81(m，4H)，3.75(m，1H)，3.70-3.56(m，2H)，3.47(dd，J＝8.5，5.3Hz，1H)，3.27(m，2H)，2.53(m，1H)，1.91(m，1H)，1.61(m，1H)；MS(ESI(+))m/e 368(M+H)+。
Example 577
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide
The title compound was prepared as described in example 132 using 5-cyano-N- {4- [ (cyclopentylacetyl) amino ]Phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of 5-cyano-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxylic acid amide.1H NMR(300MHz，DMSO-d6)δppm 9.69(s，1H)，8.31(s，1H)，7.98(s，1H)，7.87-7.78(m，2H)，7.53-7.38(m，5H)，7.36(brs，1H)，4.78(bs，4H)，2.32-2.13(m，3H)，1.82-1.67(m，2H)，1.67-1.42(m，4H)，1.27-1.10(m，2H)；MS(ESI(+))m/e 407(M+H)+。
Example 578
N- [4- ({ benzyl [3- (morpholin-4-yl) propyl ] amino } methyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
To the N- (4- { benzyl [3- (morpholin-4-yl) propyl group]To a stirred suspension of carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxamide (0.028g, 0.056mmol) in THF (1.1ml) was added dropwise 1M borane-tetrahydrofuran complex (0.225ml, 0.225 mmol). The mixture was heated at 60 ℃ for 5 hours. Additional borane complex (0.084ml) was added and the reaction was heated at 60 ℃ for 1 hour. The reaction was cooled to ambient temperature and 0.3mL of 1.25 MHCl/methanol was added. The quenched reaction was stirred for 30 min and concentrated. After flash chromatography, the title compound was isolated.1H NMR (400MHz, pyridine-d)5Temperature 90 ℃) δ ppm 8.05(s, 1H), 7.88-7.82(m, 2H), 7.47-7.38(m, 4H), 7.36-7.29(m, 2H), 7.26-7.15(m, 5H), 4.85(bs, 4H), 3.68-3.59(m, 8H), 3.48-3.35(m, 1H), 2.59(t, J ═ 7.0Hz, 2H), 2.38-2.29(m, 6H), 1.79-1.65(m, 3H); MS (ESI (+)) M/e 485(M + H) +。
Example 579
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm13.30(bs，0.25H)，12.87(bs，0.75H)，9.69(s，1H)，8.34-8.23(m，1H)，7.83-7.63(m，3H)，7.56-7.32(m，5H)，6.76-6.68(m，1H)，4.81-4.72(m，4H)，2.31-2.12(m，3H)，1.85-1.67(m，2H)，1.67-1.42(m，4H)，1.29-1.10(m，2H)；MS(ESI(+))m/e 430(M+H)+。
Example 580
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting pyridin-3-ylboronic acid for 1H-pyrazol-3-ylboronic acid and 5-bromo-N- (4- (2-cyclopentylacetamido) phenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 9.70(bs，1H)，8.93-8.89(m，1H)，8.58(dd，J＝4.7，1.6Hz，1H)，8.33(s，1H)，8.13-8.05(m，1H)，7.72(bs，1H)，7.71-7.64(m，1H)，7.54-7.44(m，6H)，4.81(bs，4H)，2.31-2.18(m，3H)，1.82-1.68(m，2H)，1.68-1.43(m，4H)，1.26-1.11(m，2H)；MS(ESI(+))m/e 441(M+H)+。
Example 581
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-methyl-1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting 1-methyl-4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -1H-pyrazole for 1H-pyrazol-3-ylboronic acid and 5-bromo-N- (4- (2-cyclopentylacetylamino) phenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide. 1H NMR(300MHz，DMSO-d6)δppm 9.69(s，1H)，8.27(s，1H)，8.14(s，1H)，7.88-7.85(m，1H)，7.55-7.40(m，6H)，7.36-7.30(m，1H)，4.77-4.69(m，4H)，3.86(s，3H)，2.31-2.16(m，3H)，1.81-1.68(m，2H)，1.68-1.42(m，4H)，1.28-1.12(m，2H)；MS(ESI(+))m/e 444(M+H)+。
Example 582
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-methoxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide
Preparation of the target as described in example 1CThe title compound, in which 2-methoxyethylamine was used instead of 3-phenylpropan-1-amine, 2- ({4- [ (cyclopentylacetyl) amino]Phenyl } carbamoyl) isoindoline-5-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 9.69(s，1H)，8.56-8.49(m，1H)，8.31(s，1H)，7.84-7.77(m，2H)，7.50-7.40(m，5H)，4.78(bs，4H)，3.50-3.39(m，4H)，3.27(s，3H)，2.31-2.18(m，3H)，1.81-1.68(m，2H)，1.66-1.43(m，4H)，1.26-1.12(m，2H)；MS(ESI(+))m/e 465(M+H)+。
Example 583
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide
The title compound was prepared as described in example 1C, substituting 2-aminoethanol for 3-phenylpropan-1-amine, 2- ({4- [ (cyclopentylacetyl) amino]Phenyl } carbamoyl) isoindoline-5-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 9.70(s，1H)，8.51-8.40(m，1H)，8.31(s，1H)，7.86-7.75(m，2H)，7.51-7.36(m，5H)，4.78(bs，4H)，4.71(t，J＝5.6Hz，1H)，3.58-3.46(m，2H)，3.39-3.28(m，2H)，2.32-2.13(m，3H)，1.82-1.68(m，2H)，1.67-1.44(m，4H)，1.27-1.10(m，2H)；MS(ESI(+))m/e 451(M+H)+。
Example 584
5- (aminomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 276 using 5-cyano-N- {4- [ (cyclopentylacetyl) amino]Phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of 5-cyano-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxylic acid amide. 1H NMR(300MHz，DMSO-d6)δppm 9.35(bs，1H)，7.99(bs，1H)，7.44-7.41(m，4H)，7.31-7.20(m，3H)，4.72(bs，4H)，3.81-3.68(m，2H)，2.29-2.25(m，3H)，1.80-1.68(m，2H)，1.66-1.48(m，6H)，1.29-1.14(m，2H)；MS(ESI(+))m/e 393(M+H)+。
Example 605
N- [6- (benzoylamino) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 605A
6- (isoindoline-2-carboxamido) hexylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 344A, substituting tert-butyl 6-aminohexylcarbamate for tert-butyl 5-aminoisoindoline-2-carboxylate.
Example 605B
N- (6-aminohexyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D, substituting Boc-6- (isoindoline-2-carboxamido) hexylcarbamic acid tert-butyl ester for 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamic acid tert-butyl ester.
Example 605C
N- [6- (benzoylamino) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (6-aminohexyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and benzoic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.42(t，J＝5.35Hz，1H)7.76-7.90(m，2H)7.36-7.58(m，3H)7.20-7.36(m，4H)6.28(t，J＝5.55Hz，1H)4.57(s，4H)3.21-3.30(m，2H)3.07(q，J＝6.74Hz，2H)1.24-1.66(m，8H)；(ESI(+))m/e 366(M+H)+。
Table 10.
The following examples were prepared as described in example 1C, substituting N- (6-aminohexyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 607
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting pyridin-4-ylboronic acid for 1H-pyrazol-3-ylboronic acid and 5-bromo-N- (4- (2-cyclopentylacetamido) phenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 9.70(s，1H)，8.69-8.61(m，2H)，8.33(s，1H)，7.82-7.69(m，4H)，7.54-7.41(m，5H)，4.81(bs，4H)，2.31-2.15(m，3H)，1.82-1.68(m，2H)，1.68-1.43(m，4H)，1.26-1.11(m，2H)；MS(ESI(+))m/e 441(M+H)+。
Example 608
5- (hydroxymethyl) -N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 4-amino-N-propylbenzamide with 4-amino-N-isoamylbenzamide and isoindolin-5-ylcarbinol hydrochloride with isoindoline-5-carboxylic acid methyl ester hydrochloride.1H NMR(300MHz，DMSO-d6)δppm8.55(s，1H)，8.24-8.17(m，1H)，7.79-7.72(m，2H)，7.68-7.61(m，2H)，7.37-7.21(m，3H)，5.19(t，J＝5.7Hz，1H)，4.76(bs，4H)，4.52(d，J＝5.7Hz，2H)，3.30-3.21(m，2H)，1.70-1.54(m，1H)，1.47-1.36(m，2H)，0.90(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 382(M+H)+。
Example 609
N- {3- [ (1-benzoylpiperidin-4-yl) oxy ] propyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 609A
4- (3- (isoindoline-2-carboxamido) propoxy) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 344A, substituting tert-butyl 4- (3-aminopropoxy) piperidine-1-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate.
Example 609B
N- (3- (piperidin-4-yloxy) propyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D substituting 4- (3- (isoindoline-2-carboxamido) propoxy) piperidine-1-carboxylic acid tert-butyl ester for 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.
Example 609C
N- {3- [ (1-benzoylpiperidin-4-yl) oxy ] propyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride and N- (3- (piperidin-4-yloxy) propyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 7.21-7.50(m，9H)6.27(t，J＝5.43Hz，1H)4.57(s，4H)3.40-3.58(m，6H)3.07-3.21(m，2H)1.74-1.93(br m，2H)1.62-1.75(m，2H)1.44(br m，2H)；MS(ESI(+))m/e 408(M+H)+。
Example 610
N- (3- { [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] oxy } propyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting nicotinoyl chloride for acetyl chloride and N- (3- (piperidin-4-yloxy) propyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 8.51-8.70(m，2H)7.75-7.88(m，1H)7.46(dd，J＝7.73，4.96Hz，1H)7.20-7.38(m，3H)6.28(t，J＝5.35Hz，1H)4.57(s，4H)3.83-4.01(m，1H)3.40-3.63(m，6H)3.16(q，J＝6.35Hz，2H)1.35-1.95(m，7H)；MS(ESI(+))m/e 409(M+H)+。
Table 11.
The following example was prepared essentially as in example 1C, substituting N- (6- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-3-yl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the corresponding carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 611
N- (6- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 611A
6-Aminopyridazine-3-carboxylic acid methyl ester
To 6-chloropyridazin-3-amine (32g, 248mmol), Et3To a solution of N (75ml, 744mmol) in MeOH (500ml) was added Pd (dppf) Cl2(12g，164mmol) and the mixture was heated at 60 ℃ under a CO atmosphere at 50psi overnight. After cooling to room temperature, the reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The residue was washed with MeOH, and the precipitate was dried under high vacuum to give the title compound as a solid.
Example 611B
6-Isocyanatopyridazine-3-carboxylic acid methyl ester
To a solution of methyl 6-aminopyridazine-3-carboxylate (14g, 91.5mmol) in dry toluene (700mL) was added Et3N (11.1, 109.8 mmol). A solution of triphosgene (27.2g, 91.5mmol) in dry toluene was slowly added at 0 ℃. The reaction mixture was stirred at room temperature for 2 hours and then heated at 90 ℃ for 5 hours. After cooling to room temperature, toluene and water were added to the mixture, the mixture was separated, and the organic layer was washed with anhydrous Na2SO4Dried and concentrated under reduced pressure to give the title compound as a solid.
Example 611C
6- (isoindoline-2-carboxamido) pyridazine-3-carboxylic acid methyl ester
To a solution of methyl 6-isocyanatopyridazine-3-carboxylate (5.26g, 29.4mmol) in THF (100ml) at 0 deg.C was added a solution of isoindoline (5.24g, 4.41mmol) in THF (50 ml). The reaction mixture was stirred at room temperature overnight. The reaction mixture was filtered, and the precipitate was washed with cold EtOAc and dried under high vacuum to give the title compound as a solid.
Example 611D
6- (isoindoline-2-carboxamido) pyridazine-3-carboxylic acid
To a solution of methyl 6- (isoindoline-2-carboxamido) pyridazine-3-carboxylate (3.7g, 12.4mmol) in MeOH (40ml) and THF (40m1) was added a solution of LiOH (0.7g, 29.2mmol) in water (10ml) at room temperature. The reaction mixture was stirred at room temperature overnight. The reaction mixture was poured into water (100ml), extracted with EtOAc (2 × 50ml) and the aqueous layer was acidified to pH3 by the addition of 2n hcl to give a precipitate. The precipitate was washed with water and dried under high vacuum to give the title compound.
Example 611E
N- (6- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting (S) - (tetrahydrofuran-3-yl) methylamine for 3-phenylprop-1-amine, and 6- (isoindoline-2-carboxamido) pyridazine-3-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid. 1H NMR(300MHz，DMSO-d6)δ9.94(s，1H)，9.12(t，J＝6.1Hz，1H)，8.31(d，J＝9.3Hz，1H)，8.11(d，J＝9.3Hz，1H)，7.41-7.28(m，4H)，4.89(s，4H)，3.80-3.55(m，3H)，3.50(dd，J＝8.5，5.2Hz，1H)，3.37-3.31(m，2H)，2.63-2.51(m，1H)，2.01-1.85(m，1H)，1.71-1.55(m，1H)；MS(ESI(+))m/e 368(M+H)+。
Example 612
N- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting cyclopentylmethylamine for 3-phenylpropan-1-amine, and 6- (isoindoline-2-carboxamido) pyridazine-3-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ9.97(s，1H)，9.00(t，J＝6.1Hz，1H)，8.31(d，J＝9.3Hz，1H)，8.11(d，J＝9.3Hz，1H)，7.41-7.28(m，4H)，5.13-4.72(m，4H)，3.31-3.16(m，2H)，2.22(p，J＝7.3Hz，1H)，1.70-1.45(m，6H)，1.38-1.20(m，2H)；MS(ESI(+))m/e 366(M+H)+。
Example 616
5- (hydroxymethyl) -N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1A, substituting (4-isocyanatobutyl) benzene for 4-isocyanatoAcid methyl benzoate, isoindolin-5-ylmethanol hydrochloride instead of isoindoline.1H NMR(300MHz，DMSO-d6)δppm 7.32-7.12(m，8H)，6.32-6.24(m，1H)，5.16(t，J＝5.6Hz，1H)，4.54(bs，4H)，4.49(d，J＝5.7Hz，2H)，3.14-3.05(m，2H)，2.64-2.54(m，2H)，1.63-1.39(m，4H)；MS(ESI(+))m/e 325(M+H)+。
Example 617
5- (hydroxymethyl) -N- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 1-isopentyl-1H-pyrazol-4-amine dihydrochloride for 4-amino-N-propylbenzamide and isoindolin-5-ylcarbinol hydrochloride for isoindoline-5-carboxylic acid methyl ester hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.39(s，1H)，7.73(s，1H)，7.39(s，1H)，7.34-7.18(m，3H)，5.19(t，J＝5.6Hz，1H)，4.67(bs，4H)，4.51(d，J＝5.5Hz，2H)，4.04(t，J＝7.1Hz，2H)，1.71-1.55(m，2H)，1.55-1.33(m，1H)，0.89(d，J＝6.5Hz，6H)；MS(ESI(+))m/e 329(M+H)+。
Example 618
N- {5- [ (3-methylbutyl) carbamoyl ] pyrazin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 618A
5- (isoindoline-2-carboxamido) pyrazine-2-carboxylic acid ethyl ester
The title compound was prepared as described in example 344A, substituting 5-aminopyrazine-2-carboxylic acid ethyl ester for 5-aminoisoindoline-2-carboxylic acid tert-butyl ester.
Example 618B
5- (isoindoline-2-carboxamido) pyrazine-2-carboxylic acid
The title compound was prepared as described in example 1B substituting 5- (isoindoline-2-carboxamido) pyrazine-2-carboxylic acid ethyl ester for 4- (isoindoline-2-carboxamido) benzoic acid methyl ester.
Example 618C
N- {5- [ (3-methylbutyl) carbamoyl ] pyrazin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 5- (isoindoline-2-carboxamido) pyrazine-2-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6Temperature 90 ℃) δ ppm 9.34(bs, 1H), 9.17(d, J ═ 1.4Hz, 1H), 8.82(d, J ═ 1.4Hz, 1H), 8.30-8.23(m, 1H), 7.36-7.26(m, 4H), 4.86(bs, 4H), 3.37-3.30(m, 2H), 1.69-1.58(m, 1H), 1.50-1.44(m, 2H), 0.92(d, J ═ 6.5Hz, 6H); MS (ESI (+)) M/e 354(M + H)+。
Example 621
N- (4- { (1E) -3- [ benzyl (methyl) amino ] prop-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 621A
(E) -N-benzyl-N-methyl-3- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) prop-2-en-1-amine
In a 4mL vial, (E) -2- (3-chloroprop-1-enyl) -4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolane (0.195mL, 0.988mmol) and potassium carbonate (273mg, 1.975mmol) were combined in dry acetonitrile (2 mL). Benzylmethylamine (0.166ml, 1.284mmol) was added to the mixture and the reaction was stirred vigorously at room temperature overnight. The reaction was diluted with ethyl acetate and washed with water and brine. The organic layer was dried over sodium sulfate, decanted, and concentrated to provide the title compound.
Example 621B
N- (4- { (1E) -3- [ benzyl (methyl) amino ] prop-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting (E) -N-benzyl-N-methyl-3- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) prop-2-en-1-amine for 1H-pyrazol-3-ylboronic acid and N- (4-bromophenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ ppm 8.12(s, 1H), 7.52(m, 2H), 7.37-7.18(m, 11H), 6.48(d, J ═ 15.8Hz, 1H), 6.18(dt, J ═ 15.8, 6.5Hz, 1H), 4.77(s, 4H), 3.53(s, 2H), 3.15(dd, J ═ 6.5, 1.4Hz, 2H), 2.18(s, 3H); MS (ESI (+)) M/e 398(M + H) +。
Example 622
N- [4- (4-phenoxypiperidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 622A
1- (4-Nitrophenyl) -4-phenoxypiperidine
A solution of 1-fluoro-4-nitrobenzene (0.15g, 1.063mmol) and 4-phenoxypiperidine hydrochloride (0.250g, 1.169mmol) in dimethylformamide (2.126ml) was treated with potassium carbonate (0.367g, 2.66 mmol). The suspension was stirred at ambient temperature for 2 hours, at 55 ℃ for 4 hours and at ambient temperature for 16 hours. The reaction was poured into water and the suspension was filtered and dried in vacuo to provide the title compound.
Example 622B
4- (4-phenoxypiperidin-1-yl) anilines
The title compound was prepared as described in example 272A, substituting 1- (4-nitrophenyl) -4-phenoxypiperidine for 4-nitro-N-propylbenzamide.
Example 622C
N- [4- (4-phenoxypiperidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 4- (4-phenoxypiperidin-1-yl) aniline for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.11(s，1H)，7.42-7.24(m，8H)，7.02-6.86(m，5H)，4.74(bs，4H)，4.59-4.47(m，1H)，3.49-3.39(m，2H)，3.03-2.91(m，2H)，2.11-1.98(m，2H)，1.81-1.66(m，2H)；MS(ESI(+))m/e 414(M+H)+。
Example 623
N- [4- (3-phenoxyazetidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 622, substituting 3-phenoxyazetidine for 4-phenoxypiperidine hydrochloride in example 622A.1H NMR(300MHz，DMSO-d6)δppm 8.06(s，1H)，7.44-7.25(m，8H)，7.03-6.93(m，1H)，6.92-6.85(m，2H)，6.47-6.40(m，2H)，5.19-5.08(m，1H)，4.73(bs，4H)，4.32-4.23(m，2H)，3.69(dd，J＝8.2，4.2Hz，2H)；MS(ESI(+))m/e386(M+H)+。
Example 624
N- (4- { [ benzyl (methyl) amino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
A suspension of isoindoline (0.1g, 0.839mmol) and N-ethyl-N-isopropylpropan-2-amine (0.219ml, 1.259mmol) in acetonitrile (2.80ml) was treated with N-methylpyrrolidine (2.80 ml). The solution was cooled to 0 ℃ and 1- (chloromethyl) -4-isocyanatobenzene (0.155g, 0.923mmol) was added. After stirring at 0 ℃ for 2h, the reaction was treated with a solution of N-methyl-1-phenylmethylamine (0.102g, 0.839mmol) in 0.5ml acetonitrile. The reaction was stirred at 0 ℃ for 5 minutes and at ambient temperature for 30 minutes. The reaction was treated with water and the mixture was stirred for 4 hours. The suspension was filtered and the collected solid was washed with water and dried in vacuo to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 8.31(s，1H)，7.56-7.49(m，2H)，7.40-7.28(m，8H)，7.27-7.19(m，3H)，4.76(bs，4H)，3.47(s，2H)，3.43(s，2H)，2.06(s，3H)；MS(ESI(+))m/e 372(M+H)+。
Example 625
5-fluoro-N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 410 using 5-fluoro-N- (4- { [ tetrahydrofuran-3-ylmethyl)]Carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide for N- (4- { [ tetrahydrofuran-3-ylmethyl ]Carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide.1H NMR(300MHz，DMSO-d6)δ8.60(s，1H)8.39(t，J＝5.7Hz，1H)，7.81-7.73(m，2H)，7.69-7.62(m，2H)，7.40(dd，J＝8.4，5.2Hz，1H)，7.24(dd，J＝9.1，2.5Hz，1H)，7.15(td，J＝8.9，2.5Hz，1H)，4.80-4.72(m，4H)，3.80-3.68(m，1H)，3.68-3.56(m，2H)，3.47(dd，J＝8.5，5.2Hz，2H)，3.21(dt，J＝13.3，5.9Hz，2H)，2.01-1.86(m，1H)，1.67-1.53(m，1H)；MS(ESI(+))m/e 384(M+H)+。
Example 626
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 411 with 5-fluoro-N- (4- { [ tetrahydrofuran-3-ylmethyl)]Carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide for N- (4- { [ tetrahydrofuran-3-ylmethyl]Carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide.1H NMR(300MHz，DMSO-d6)δ8.60(s，1H)，8.39(t，J＝5.7Hz，1H)，7.80-7.73(m，2H)，7.69-7.62(m，2H)，7.40(dd，J＝8.4，5.2Hz，1H)，7.24(dd，J＝9.1，2.5Hz，1H)，7.15(td，J＝8.9，2.5Hz，1H)，4.80-4.73(m，4H)，3.80-3.56(m，3H)，3.47(dd，J＝8.5，5.2Hz，1H)，3.24-3.13(m，2H)，2.01-1.86(m，1H)，1.67-1.53(m，1H)；MS(ESI(+))m/e 384(M+H)+。
Example 636
N- [4- (1-benzyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 636A
N- (4-ethynylphenyl) isoindoline-2-carboxamide
The title compound was prepared as described in example 1A, substituting 1-ethynyl-4-isocyanatobenzene for methyl 4-isocyanatobenzoate.
Example 636B
N- [4- (1-benzyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
A mixture of N- (4-ethynylphenyl) isoindoline-2-carboxamide (100mg, 0.381mmol), benzylamine (33.2mg, 0.381mmol) and sodium ascorbate (15mg, 0.076mmol) in methanol (1.9ml) was treated with 1H-imidazole-1-sulfonyl azide hydrochloride (66.0mg, 0.381mmol), copper (II) sulfate pentahydrate (9.52mg, 0.038mmol) and triethylamine (63.8. mu.l, 0.457 mmol). Additional methanol (2mL) was added and the vial was purged with nitrogen and stirred for 2 days. The mixture was diluted with water and the resulting suspension was filtered and washed with water to provide the title compound as a white solid. 1H NMR(300MHz，DMSO-d6)δ8.51(s，1H)，8.45(s，1H)，7.73(d，J＝8.7Hz，2H)，7.65(d，J＝8.9Hz，2H)，7.49-7.24(m，9H)，5.63(s，2H)，4.78(s，4H)，1.11-1.00(m，1H)；MS(ESI(+))m/e396(M+H)+。
Table 12.
The following examples are prepared essentially as described in example 636B, substituting the appropriate amine for benzylamine.
Example 646
N- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
In a 50ml pressure bottle, N- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide (50mg, 0.128mmol) and methanol (10ml) were added to 5% Pd-C (wet, 10.00mg, 0.094mmol) and stirred at 30psi at room temperature for 16 h. The mixture was filtered through a nylon membrane and concentrated. Chromatography was performed to provide the title compound.1H NMR(500MHz，DMSO-d6)δppm 8.60(s，1H)，8.50(d，J＝5.0Hz，1H)，8.35(s，1H)，7.49-7.40(m，3H)，7.13(m，2H)，4.79(m，4H)，4.56(m，1H)，4.05(m，1H)，3.12(m，1H)，2.90(m，1H)，2.71(m，1H)，2.57(m，1H)，1.79(m，2H)，1.55-1.30(m，2H)，1.02(m，6H)；MS(ESI(+))m/e 393(M+H)+。
Example 647
N- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 646 using N- (4- {1- [ (2-methoxyethoxy) acetyl]-1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of N- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(500MHz，DMSO-d6)δppm8.27(s，1H)，7.47(m，2H)，7.39-7.28(m，4H)，7.12(m，2H)，4.75(bs，4H)，4.47(m，1H)，4.24-4.09(m，2H)，3.90(m，1H)，3.57(m，2H)，3.47(t，J＝4.7Hz，2H)，3.26(s，3H)，3.06(m，1H)，2.70(m，1H)，2.62(m，1H)，1.77(m，2H)，1.57(m，1H)，1.42(m，1H)；MS(ESI(+))m/e 438(M+H)+。
Example 648
N- {5- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 646 using N- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide for N- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(500MHz，DMSO-d6)δppm 8.81(s，1H)，8.16(d，J＝2.4Hz，1H)，7.85(d，J＝8.6Hz，1H)，7.63(dd，J＝8.7，2.4Hz，1H)，7.39-7.25(m，4H)，4.80(s，4H)，4.56(d，J＝13.1Hz，1H)，4.08(d，J＝12.3Hz，1H)，3.88(m，1H)，3.72(m，3H)，3.38(m，1H)，3.11(m，1H)，2.78(dd，J＝11.9，9.2Hz，1H)，2.63(m，1H)，2.03(m，2H)，1.80(t，J＝15.4Hz，2H)，1.51(m，2H)；MS(ESI(+))m/e 421(M+H)+。
Example 651
N- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 651A
N- (6-chloropyridin-3-yl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 1A substituting 2-chloro-5-isocyanatopyridine for methyl 4-isocyanatobenzoate and 2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine for isoindoline.
Example 651B
4- (5- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) pyridin-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester
The title compound was prepared as described in example 280, using tert-butyl 4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylate instead of 1H-pyrazol-3-ylboronic acid and N- (6-chloropyridin-3-yl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.
Example 651C
N- (6- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-3-yl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 2D, substituting 4- (5- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) pyridin-2-yl) -5, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester for 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.
Example 651D
N- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting N- (6- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-3-yl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and isobutyric acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(501MHz，DMSO-d6Temperature 90 ℃) δ ppm 8.73(d, J ═ 2.6Hz, 1H), 8.64(s, 1H), 8.52(m, 2H), 7.99(dd, J ═ 8.6, 2.6Hz, 1H), 7.49(d, J ═ 8.7Hz, 1H), 7.44(d, J ═ 5.0Hz, 1H), 6.60(m, 1H), 4.88(bs, 2H), 4.85(d, J ═ 2.3Hz, 2H), 4.22(m, 2H), 3.73(t, J ═ 5.7Hz,2H)，2.96(m，1H)，2.63(m，2H)，1.08(d，J＝6.7Hz，6H)；MS(ESI(+))m/e 392(M+H)+。
table 13.
The following example was prepared essentially as in example 1C, substituting N- (6- (1, 2, 3, 6-tetrahydropyridin-4-yl) pyridin-3-yl) -1H-pyrrolo [3, 4-C ] pyridine-2 (3H) -carboxamide for 3-phenylpropan-1-amine and the corresponding carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 699
N- {4- [1- (pyridin-2-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting picolinoyl chloride for acetyl chloride, N- [4- (piperidin-4-yl) butyl]-1, 3-dihydro-2H-isoindole-2-carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(300MHz，DMSO-d6)δppm 8.56(d，J＝4.76Hz，1H)7.83-7.97(m，1H)7.38-7.57(m，2H)7.18-7.40(m，4H)6.27(t，J＝5.55Hz，1H)4.56(s，4H)4.47(d，J＝13.09Hz，1H)3.59(d，J＝13.88Hz，1H)3.00-3.16(m，3H)2.92-3.01(m，1H)2.68-2.81(m，1H)1.77(d，J＝12.69Hz，1H)0.97-1.64(m，11H)；MS(ESI(+))m/e 407(M+H)+。
Example 718
N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 718A
(tetrahydrofuran-3-yl) methylcarbamic acid benzyl ester
Racemic (tetrahydrofuran-3-yl) methylamine (3.84g, 38.0mmol) and diisopropylethylamine (13.26ml, 76mmol) were dissolved in dichloromethane (100ml) and cooled to 0 ℃. The mixture was treated dropwise with benzyl chloroformate (6.19ml, 41.8mmol) dissolved in 30ml of dichloromethane via an addition funnel. After addition, the cooling bath was removed and the homogeneous solution was stirred at ambient temperature overnight. The reaction mixture was partitioned between water and ethyl acetate, and the separated aqueous layer was extracted with ethyl acetate. The combined organic layers were washed with brine, dried over magnesium sulfate, filtered, and concentrated. Chromatography was performed to provide the title compound.
Example 718B
(S) - (tetrahydrofuran-3-yl) methyl carbamic acid benzyl ester
The racemic mixture of benzyl (tetrahydrofuran-3-yl) methylcarbamate was dissolved in tetrahydrofuran, separated by liquid chromatography (Chiralpak IC 2.5cm ID x 25cm, 20 micron column), eluting with hexane/tetrahydrofuran/isopropanol (85/10/5), to provide benzyl (R) - (tetrahydrofuran-3-yl) methylcarbamate and benzyl (S) - (tetrahydrofuran-3-yl) methylcarbamate.
Example 718C
(S) - (tetrahydrofuran-3-yl) methylamine
Benzyl (R) - (tetrahydrofuran-3-yl) methylcarbamate (8.9g, 37.8mmol) and ethanol (160mL) were added to 20% wet palladium (II) hydroxide (0.890g, 6.34mmol) in a 250mL stainless steel pressure bottle and stirred at 30psi at room temperature for 40 minutes. The mixture was filtered through a nylon filter and acidified with 4N HCl/dioxane (5 eq). Concentration and drying provided the title compound.
Example 718D
N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting (S) - (tetrahydrofuran-3-yl) methylamine for 3-phenylpropan-1-amine, 4- (2, 3-dihydro-1H-pyrrolo [3, 4-C) ]Pyridine-2-carboxamido) benzoic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.64(s，2H)，8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.38(t，J＝5.7Hz，1H)，7.81-7.74(m，2H)，7.69-7.62(m，2H)，7.44(d，J＝5.1Hz，1H)，4.86-4.79(m，4H)，3.80-3.66(m，2H)，3.67-3.56(m，1H)，3.47(dd，J＝8.5，5.3Hz，1H)，3.21(dt，J＝13.2，5.8Hz，1H)，2.01-1.86(m，1H)，1.67-1.53(m，1H)；MS(ESI(+))m/e 367(M+H)+。
Example 720
N- (7-oxo-7- { [ (3R) -tetrahydrofuran-3-ylmethyl ] amino } heptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 720A
7- (isoindoline-2-carboxamido) heptanoic acid methyl ester
The title compound was prepared as described in example 344A substituting methyl 7-aminoheptanoate for tert-butyl 5-aminoisoindoline-2-carboxylate.
Example 720B
7- (isoindoline-2-carboxamido) heptanoic acid
The title compound was prepared as described in example 1B substituting methyl 7- (isoindoline-2-carboxamido) heptanoate for methyl 4- (isoindoline-2-carboxamido) benzoate.
Example 720C
N- (7-oxo-7- { [ (3R) -tetrahydrofuran-3-ylmethyl ] amino } heptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting (R) - (tetrahydrofuran-3-yl) methylamine for 3-phenylpropan-1-amine and 7- (isoindoline-2-carboxamido) heptanoic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm7.85(t，J＝5.76Hz，1H)7.20-7.37(m，4H)6.26(t，J＝5.59Hz，1H)4.57(s，4H)3.49-3.79(m，3H)3.35(dd，J＝8.48，5.43Hz，1H)2.94-3.15(m，4H)2.18-2.38(m，1H)2.05(t，J＝7.29Hz，2H)1.79-1.98(m，1H)1.35-1.60(m，7H)1.17-1.35(m，2H)；MS(ESI(+))m/e 374(M+H)+。
Example 721
N- { 7-oxo-7- [ (tetrahydro-2H-pyran-4-ylmethyl) amino ] heptyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting (tetrahydro-2H-pyran-4-yl) methylamine for 3-phenylpropan-1-amine and 7- (isoindoline-2-carboxamido) heptanoic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm7.76(t，J＝5.75Hz，1H)7.20-7.40(m，4H)6.26(t，J＝5.55Hz，1H)4.57(s，4H)3.82(dd，J＝11.10，2.78Hz，2H)3.14-3.29(m，2H)3.05(q，J＝6.74Hz，2H)2.92(t，J＝6.15Hz，2H)2.06(t，J＝7.54Hz，2H)1.33-1.65(m，9H)1.19-1.34(m，2H)0.98-1.22(m，2H)；MS(ESI(+))m/e 388(M+H)+。
Example 722
N- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 722A
4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) butyl) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 344, substituting 4- (4-aminobutyl) piperidine-1-carboxylic acid tert-butyl ester for 5-aminoisoindoline-2-carboxylic acid tert-butyl ester and 1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine for isoindoline in example 344A.
Example 722B
N- (4- (piperidin-4-yl) butyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 2D, substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) butyl) piperidine-1-carboxylate. Example 722C
N- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, using N- (4- (piperidin-4-yl) butyl) -1H-pyrrolo [3, 4-C ]]Pyridine-2 (3H) -carboxamide replaces 3-phenylpropan-1-amine, and benzoic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(500MHz，DMSO-d6Temperature 90 ℃) δ ppm 8.54(s, 1H)8.45(d, J ═ 5.04Hz, 1H)7.38-7.46(m, 3H)7.28-7.37(m, 3H)6.09(s, 1H)4.62(dd, J ═ 9.08, 1.60Hz, 4H)3.07-3.15(m, 2H)2.79-2.94(m, 2H)1.61-1.75(m, 2H)1.41-1.58(m, 3H)1.20-1.40(m, 4H)0.99-1.17(m, 2H); MS (ESI (+)) M/e 407(M + H)+。
Table 14.
The following examples were prepared essentially as described in example 722C, substituting the appropriate carboxylic acid for benzoic acid.
Example 753
N- {4- [5- (morpholin-4-ylmethyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 753A
N- (4- (5- (chloromethyl) -1, 2, 4-oxadiazol-3-yl) phenyl) isoindoline-2-carboxamide
To a 25mL round bottom flask containing (z) -N- (4- (N' -hydroxycarbamimidoyl) phenyl) isoindoline-2-carboxamide (1.5g, 5.06mmol) (in acetone (5 mL)) was added potassium carbonate (7.00g, 50.6mmol) in one portion. The reaction mixture was cooled to 0 ℃ and 2-chloroacetyl chloride (3.22ml, 40.5mmol) was added slowly. The resulting mixture was warmed to room temperature and stirred for two hours. The solvent was removed and the solid was triturated with water, then filtered and washed with water. The dried solid was dissolved in DMF, heated to 100 ℃ and stirred for two hours. Work-up with water and dichloromethane followed by chromatography afforded the title compound.
Example 753B
N- {4- [5- (morpholin-4-ylmethyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
To a 20ml vial was added N- (4- (5- (chloromethyl) -1, 2, 4-oxadiazol-3-yl) phenyl) isoindoline-2-carboxamide (50mg, 0.141mmol) and morpholine (36.8mg, 0.423mmol) (in DMF (470. mu.l)). The mixture was heated to 50 ℃ for 30 minutes, cooled and diluted with 2mL of methanol. Chromatography was performed to provide the title compound.1H NMR(300MHz，DMSO-d6)δ8.69(s，1H)，7.92(d，J＝8.8Hz，2H)，7.80(d，J＝8.9Hz，2H)，7.35(ddd，J＝8.8，3.9，2.4Hz，4H)，4.80(s，4H)，3.95(s，2H)，3.68-3.48(m，4H)，2.62-2.51(m，5H)；MS(ESI(+))m/e406(M+H)+。
Example 754
N- (4- {5- [ (4-methylpiperazin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 753B, substituting 1-methylpiperazine for morpholine.1H NMR(300MHz，DMSO-d6)δ8.69(s，1H)，7.91(d，J＝8.8Hz，3H)，7.80(d，J＝8.8Hz，3H)，7.45-7.23(m，5H)，4.80(s，5H)，3.93(s，2H)，2.65-2.51(m，75H)，2.34(s，5H)，2.15(s，4H)；MS(ESI(+))m/e419(M+H)+。
Example 755
N- [4- (5- { [ (3-methylbutyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 753B, substituting 3-methylbutan-1-amine for morpholine.1H NMR(300MHz，DMSO-d6)δppm 8.68(s，1H)，7.91(d，J＝8.8Hz，2H)，7.79(d，J＝8.8Hz，2H)，7.35(tdd，J＝8.9，5.4，3.4Hz，4H)，4.80(s，4H)，4.02(s，2H)，2.66-2.53(m，1H)，2.43-2.30(m，1H)，1.63(dt，J＝13.4，6.7Hz，1H)，1.32(dd，J＝14.4，7.0Hz，2H)，0.86(d，J＝6.5Hz，6H)；MS(ESI(+))m/e 406(M+H)+。
Example 756
N- (4- {5- [ (4-hydroxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 753B, substituting piperidin-4-ol for morpholine. 1H NMR(300MHz，DMSO-d6)δppm 8.68(s，1H)，7.91(d，J＝8.8Hz，2H)，7.79(d，J＝8.8Hz，2H)，7.45-7.25(m，4H)，4.80(s，4H)，4.56(d，J＝4.2Hz，1H)，3.91(s，2H)，3.45(dd，J＝8.7，4.3Hz，1H)，3.17(d，J＝5.2Hz，1H)，2.76(dd，J＝10.6，5.0Hz，2H)，2.42-2.18(m，3H)，1.72(d，J＝8.9Hz，2H)，1.43(dt，J＝18.5，6.4Hz，2H)；MS(ESI(+))m/e420(M+H)+。
Example 787
N- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } -2-oxoethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 787A
N-benzyl-N- (3-morpholinopropyl) -2- (4-nitrophenyl) acetamide
The title compound was prepared as described in example 1C, substituting N-benzyl-3-morpholinopropan-1-amine for 3-phenylpropan-1-amine and 2- (4-nitrophenyl) acetic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 787B
2- (4-aminophenyl) -N-benzyl-N- (3-morpholinopropyl) acetamide
The title compound was prepared as described in example 272A, substituting N-benzyl-N- (3-morpholinopropyl) -2- (4-nitrophenyl) acetamide for 4-nitro-N-propylbenzamide.
Example 787C
N- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } -2-oxoethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B using 2- (4-aminophenyl) -N-benzyl-N- (3-morpholinopropyl) acetamide in place of 4-amino-N-propylbenzamide and isoindoline in place of methyl isoindoline-5-carboxylate hydrochloride.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ ppm 8.05(bs, 1H), 7.47(d, J ═ 8.5Hz, 2H), 7.37-7.17(m, 9H), 7.15-7.08(m, 2H), 4.76(s, 4H), 4.56(bs, 2H), 3.77-3.55(m, 2H), 3.56-3.50(m, 4H), 3.30(t, J ═ 7.3Hz, 2H), 2.33-2.24(m, 4H), 2.21(t, J ═ 6.8Hz, 2H), 1.60(p, J ═ 7.1Hz, 2H); MS (ESI (+)) M/e513(M + H) +。
Example 788
N- [4- (3- { benzyl [3- (morpholin-4-yl) propyl ] amino } -3-oxopropyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 787, substituting 3- (4-nitrophenyl) propionic acid for 2- (4-nitrophenyl) acetic acid in example 787A.1H NMR(400MHz，DMSO-d6δ ppm 7.99(bs, 1H), 7.48-7.39(m, 2H), 7.37-7.19(m, 7H), 7.19-7.13(m, 2H), 7.13-7.00(m, 2H), 4.76(s, 4H), 4.53(s, 2H), 3.56-3.45(m, 4H), 3.31-3.23(m, 2H), 2.87-2.78(m, 2H), 2.72-2.57(m, 2H), 2.29-2.22(m, 4H), 2.20(t, J ═ 6.8Hz, 2H), 1.63-1.54(m, 2H); MS (ESI (+)) M/e 527(M + H)+。
Example 795
N- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting tetrahydro-2H-pyran-4-ylmethylamine for 3-phenylpropan-1-amine, and 6- (isoindoline-2-carboxamido) pyridazine-3-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ9.98(s，1H)，9.03(t，J＝6.2Hz，1H)，8.31(d，J＝9.3Hz，1H)，8.10(d，J＝9.3Hz，1H)，7.41-7.28(m，4H)，5.03-4.67(m，4H)，3.89-3.79(m，2H)，3.29-3.11(m，4H)，2.01-1.78(m，1H)，1.63-1.53(m，2H)，1.30-1.12(m，2H)；MS(ESI(+))m/e 382(M+H)+。
Example 797
N- [4- (6-bromo-2-oxoquinolin-1 (2H) -yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 797A
4- (6-bromo-2-oxoquinolin-1 (2H) -yl) butylcarbamic acid tert-butyl ester
To a solution of 6-bromoquinolin-2 (1H) -one (430mg, 1.91mmol) in tetrahydrofuran (8ml) was added sodium bis (trimethylsilyl) amide (2.1ml, 2.08 mmol). After 15 min, 4- (Boc-amino) butyl bromide (403mg, 1.6mmol) was added. The solution was stirred for 15 hours, concentrated and purified by flash chromatography to provide the title compound.
Example 797B
1- (4-aminobutyl) -6-bromoquinolin-2 (1H) -one
The title compound was prepared as described in example 2D substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (6-bromo-2-oxoquinolin-1 (2H) -yl) butylcarbamate.
Example 797C
N- [4- (6-bromo-2-oxoquinolin-1 (2H) -yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B using 1- (4-aminobutyl) -6-bromoquinolin-2 (1H) -one instead of 4-amino-N-propylbenzamide and isoindoline instead of methyl isoindoline-5-carboxylate hydrochloride.1H NMR(400MHz，CDCl3)δppm 7.67(d，J＝2.2Hz，2H)，7.61(d，J＝2.3Hz，1H)，7.60(d，J＝2.3Hz，1H)，7.57(d，J＝9.6Hz，2H)，7.28(s，1H)，7.24(s，1H)，6.70(d，J＝9.5Hz，2H)，4.76(t，J＝5.7Hz，2H)，4.70(s，4H)，4.29(m，2H)，3.42(m，2H)，1.79(m，2H)，1.69(m，2H)；MS(ESI(+))m/e 440.1(M+H)。
Example 798
N- {4- [6- (3-acetylphenyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting 3-acetylphenylboronic acid for 1H-pyrazol-3-ylboronic acid, N- [4- (6-bromo-2-oxoquinolin-1 (2H) -yl) butyl ]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide instead of 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxylic acid amide.1H NMR(400MHz，CDCl3)δppm 8.20(t，J＝1.5Hz，1H)，7.94(d，J＝7.7Hz，1H)，7.80(m，3H)，7.75(d，J＝9.5Hz，2H)，7.56(t，J＝7.7Hz，1H)，7.49(d，J＝9.4Hz，2H)，7.24(s，1H)，6.75(t，J＝9.4Hz，2H)，4.82(t，J＝5.4Hz，1H)，4.72(s，4H)，4.37(m，2H)，3.45(m，2H)，2.66(s，3H)，1.88(m，2H)，1.74(m，2H)；MS(ESI(+))m/e480.3(M+H)。
Example 804
5- (hydroxymethyl) -N- (3-phenylpropyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 3-phenylpropan-1-amine for 4-amino-N-propylbenzamide and isoindolin-5-ylcarbinol hydrochloride for isoindoline-5-carboxylic acid methyl ester hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 7.30-7.14(m，8H)，6.30(t，J＝5.5Hz，1H)，5.16(t，J＝5.5Hz，1H)，4.55(bs，4H)，4.49(d，J＝4.9Hz，2H)，3.16-3.05(m，2H)，2.64-2.56(m，2H)，1.76(p，J＝7.4Hz，2H)；MS(ESI(+))m/e 311(M+H)+。
Example 805
N- (2- { (4-Fluorobenzyl) [4- (pyridin-3-yl) benzyl ] amino } -1, 3-thiazol-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 805A
2- (4- (pyridin-3-yl) benzylamino) thiazole-5-carboxylic acid methyl ester
A250 mL round bottom flask was charged with 4- (pyridin-3-yl) benzaldehyde (4g, 21.83mmol), methyl 2-aminothiazole-5-carboxylate (3.45g, 21.83mmol) and acetic acid (0.375mL, 6.55mmol) in toluene (109 mL). The mixture was heated at reflux under Dean-Stark conditions for 3 hours, cooled, concentrated, and redissolved in methanol. The mixture was cooled to 0 ℃ and sodium borohydride (1.322g, 34.9mmol) was added carefully. The mixture was warmed to room temperature and the resulting suspension was filtered, washed with water and dried to provide the title compound.
Example 805B
2- ((4-Fluorobenzyl) (4- (pyridin-3-Yl) benzyl) amino) thiazole-5-carboxylic acid
A250 mL round bottom flask was charged with methyl 2- (4- (pyridin-3-yl) benzylamino) thiazole-5-carboxylate (3g, 9.22mmol) and 1- (bromomethyl) -4-fluorobenzene (1.264mL, 10.14mmol) in dimethylformamide (46.1 mL). The mixture was cooled to 0 ℃ and sodium hydride (0.738g, 18.44mmol) was added carefully; and the mixture was warmed to room temperature. After stirring the mixture for about 30 minutes, it was found to be predominantly carboxylic acid. Adding 1N NaOH to complete conversion; treatment with water followed by chromatography provided the title compound.
Example 805C
N- (4-fluorobenzyl) -5-isocyanato-N- (4- (pyridin-3-yl) benzyl) thiazol-2-amine
To a 50ml round bottom flask was added 2- ((4-fluorobenzyl) (4- (pyridin-3-yl) benzyl) amino) thiazole-5-carboxylic acid (850mg, 2.026mmol) in dichloromethane (10.100ml) and the solution was cooled to 0 ℃. Oxalyl chloride (0.266ml, 3.04mmol) and dimethylformamide (0.016ml, 0.203mmol) were added and some bubbling occurred. The solution was warmed to room temperature and stirred for 1 hour. The mixture was cooled to 0 ℃ and trimethylsilyl azide (0.538ml, 4.05mmol) was added. The mixture was warmed to room temperature, stirred for 30 minutes, and concentrated in vacuo. Toluene (5ml) was added and the mixture was heated to 95 ℃ for 2.5 hours. The toluene was removed and the resulting solid was triturated/sonicated with ether, filtered, and washed with ether to provide the title compound.
Example 805D
N- (2- { (4-Fluorobenzyl) [4- (pyridin-3-yl) benzyl ] amino } -1, 3-thiazol-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1A substituting N- (4-fluorobenzyl) -5-isocyanato-N- (4- (pyridin-3-yl) benzyl) thiazol-2-amine for methyl 4-isocyanatobenzoate, 1, 3-dihydro-2H-pyrrolo [3, 4-c ] p]Pyridine is substituted for isoindoline.1H NMR(300MHz，DMSO-d6)δppm 9.27(s，1H)，8.99(d，J＝2.1Hz，1H)，8.76(s，1H)，8.71-8.56(m，2H)，8.29(d，J＝7.8Hz，1H)，7.81-7.56(m，5H)，7.51-7.27(m，5H)，7.27-7.06(m，2H)，6.86(s，1H)，4.80(d，J＝3.6Hz，4H)，4.72(d，J＝7.7Hz，4H)；MS(ESI(+))m/e 537(M+H)+。
Example 806
N- [4- (2-benzyl-1, 3-thiazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 806A
4- (2-benzylthiazol-4-yl) aniline
In a 20mL microwave reaction vessel, 2-bromo-1- (4-nitrophenyl) ethanone (0.5g, 2.049mmol) and 2-phenylthioacetamide (0.310g, 2.049mmol) were mixed in ethanol (10mL) and heated at 140 ℃ for 15 minutes. The solution was transferred to a 250mL round bottom flask where it immediately solidified. The material was diluted with additional ethanol (10ml) and heated under reflux with stirring until the solid dissolved. Water (5.0ml, 278mmol) and hydrochloric acid (1ml, 12.00mmol) were added. Iron (.625g, 11.19mmol) was added and the mixture heated at reflux for 2 h. Mixing the above materialsThe mixture was cooled and 5mL NH was added4And (5) OH. The material was filtered through a pad of celite, and the pad was washed with 50mL of ethyl acetate. The filtrate was washed with 100mL of water and the aqueous phase was extracted with an additional 50mL of ethyl acetate. The combined organic fractions were dried over sodium sulfate, filtered and the solvent was removed under reduced pressure. The material was redissolved in 50mL ethyl acetate and filtered through a 1/4 inch pad of silica gel. The pad was washed with an additional 50mL of ethyl acetate and the combined filtrates were concentrated to provide the title compound.
Example 806B
N- [4- (2-benzyl-1, 3-thiazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 4- (2-benzylthiazol-4-yl) aniline for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.1H NMR(400MHz，CDCl3)δppm 7.79(d，J＝8.7Hz，2H)，7.48(d，J＝8.7Hz，2H)，7.30(s，1H)，7.29(d，J＝3.8Hz，2H)，7.26(m，5H)，7.20(d，J＝3.7Hz，2H)，6.29(s，1H)，4.80(s，4H)，4.32(s，2H)；MS(ESI(+))m/e 412(M+H)。
Example 807
N- (7- { benzyl [3- (morpholin-4-yl) propyl ] amino } -7-oxoheptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N-benzyl-3-morpholinopropan-1-amine for 3-phenylpropan-1-amine and 7- (isoindoline-2-carboxamido) heptanoic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 7.41-7.13(m，9H)，6.32-6.22(m，1H)，4.59-4.48(m，6H)，3.58-3.47(m，4H)，3.27-3.20(m，2H)，3.11-2.98(m，2H)，2.44-2.36(m，1H)，2.31-2.23(m，5H)，2.23-2.12(m，2H)，1.70-1.17(m，10H)；MS(ESI(+))m/e 507(M+H)+。
Example 808
N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 808A
N-isopentyl-4-nitrobenzenesulfonamides
4-Nitrobenzene-1-sulfonyl chloride (1.5g, 6.57mmol) was dissolved in dichloromethane (30ml) and cooled to 0 ℃ before adding diisopropylethylamine (2.293ml, 13.13 mmol). 3-Methylbutan-1-amine (0.926ml, 7.88mmol) was dissolved in 5ml of dichloromethane and added by syringe. After the addition, the mixture was warmed to room temperature and held for 3 hours. The solution was diluted with aqueous sodium bicarbonate and extracted twice with dichloromethane. The organics were combined, dried over magnesium sulfate, filtered, and concentrated. Chromatography was performed to provide the title compound.
Example 808B
4-amino-N-isopentylbenzenesulfonamides
The title compound was prepared as described in example 272A, substituting N-isopentyl-4-nitrobenzenesulfonamide for 4-nitro-N-propylbenzamide.
Example 808C
N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 4-amino-N-isopentylbenzenesulfonamide for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.75(s，1H)，7.82-7.74(m，2H)，7.70-7.64(m，2H)，7.41-7.27(m，5H)，4.80(s，4H)，2.77-2.67(m，2H)，1.64-1.47(m，1H)，1.30-1.19(m，2H)，0.79(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 388(M+H)+。
Example 839
N- (5- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting (S) - (tetrahydrofuran-3-yl) methylcarbamic acid benzyl ester for 3-phenylpropan-1-amine, and 6- (isoindoline-2-carboxamido) nicotinic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(500MHz，DMSO-d6)δppm 9.27(s，1H)，8.74(d，J＝2.1Hz，1H)，8.60(t，J＝5.7Hz，1H)，8.14(dd，J＝8.8，2.4Hz，1H)，8.00(d，J＝8.7Hz，1H)，7.41-7.27(m，4H)，4.89(m，4H)，3.75(m，1H)，3.69(m，1H)，3.62(m，1H)，3.48(dd，J＝8.5，5.3Hz，1H)，3.25(m，2H)，2.48(m，1H)，1.95(m，1H)，1.61(m，1H)；MS(ESI(+))m/e 367(M+H)。
Example 871
N- [4- (4- { benzyl [3- (morpholin-4-yl) propyl ] amino } -4-oxobutyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 787, substituting 3- (4-nitrophenyl) butanoic acid for 2- (4-nitrophenyl) acetic acid in example 787A. 1H NMR(300MHz，DMSO-d6)δppm 8.29-8.21(m，1H)，7.51-7.41(m，2H)，7.40-7.13(m，9H)，7.11-6.98(m，2H)，4.75(s，4H)，4.57-4.47(m，2H)，3.60-3.44(m，4H)，3.27-3.13(m，2H)，2.60-2.53(m，1H)，2.48-2.34(m，2H)，2.33-2.11(m，7H)，1.90-1.71(m，2H)，1.66-1.51(m，2H)；MS(ESI(+))m/e 541(M+H)+。
Example 872
N- (4-phenylbutyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1A substituting (4-isocyanatobutyl) benzene for methyl 4-isocyanatobenzoate, 1, 3-dihydro-2H-pyrrolo [3, 4-c ] or]Pyridine is substituted for isoindoline.1H NMR(300MHz，DMSO-d6)δppm 8.55(s，1H)，8.46(d，J＝5.0Hz，1H)，7.38(d，J＝5.1Hz，1H)，7.32-7.22(m，2H)，7.23-7.11(m，3H)，6.38(t，J＝5.6Hz，1H)，4.63-4.57(m，4H)，3.10-3.07(m，2H)，2.59(t，J＝7.5Hz，2H)，1.66-1.39(m，4H)；MS(ESI(+))m/e 296(M+H)+。
Example 873
N- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 873A
N-benzyl-3-morpholino-N- (4-nitrophenylethyl) propan-1-amine
A suspension of 1- (2-bromoethyl) -4-nitrobenzene (0.314g, 1.366mmol), N-benzyl-3-morpholinopropan-1-amine (0.128g, 0.546mmol) and potassium carbonate (0.189g, 1.366mmol) in dimethylformamide (1.821ml) was heated at 65 ℃ for 20 h. The reaction was partitioned between ethyl acetate and water. The organic layer was washed with brine, dried over anhydrous sodium sulfate, filtered, and concentrated. The concentrate was purified by flash chromatography to provide the title compound.
Example 873B
4- (2- (benzyl (3-morpholinopropyl) amino) ethyl) aniline
The title compound was prepared as described in example 272A, substituting N-benzyl-3-morpholino-N- (4-nitrophenylethyl) propan-1-amine for 4-nitro-N-propylbenzamide.
Example 873C
N- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B using 4- (2- (benzyl (3-morpholinopropyl) amino) ethyl) aniline instead of 4-amino-N-propylbenzamide and isoindoline instead of methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm8.24(s，1H)，7.43(d，J＝8.5Hz，2H)，7.38-7.18(m，9H)，7.04(d，J＝8.5Hz，2H)，4.75(s，4H)，3.60(s，2H)，3.54-3.47(m，4H)，2.70-2.54(m，4H)，2.48-2.41(m，2H)，2.29-2.16(m，6H)，1.62-1.46(m，2H)；MS(ESI(+))m/e 499(M+H)+。
Example 876
5-cyano-N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 4-amino-N-isopentylbenzamide for 4-amino-N-propylbenzamide and isoindoline-5-carbonitrile for methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.82(s，1H)，7.89(s，1H)，7.83-7.74(m，3H)，7.71-7.64(m，2H)，7.59(d，J＝7.9Hz，1H)，7.31(t，J＝5.8Hz，1H)，4.89-4.81(m，4H)，2.78-2.67(m，2H)，1.56(dp，J＝13.3，6.7Hz，1H)，1.30-1.19(m，2H)，0.78(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 413(M+H)+。
Example 877
N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 272B substituting 4-amino-N-isopentylbenzenesulfonamide for 4-amino-N-propylbenzamide, 1, 3-dihydro-2H-pyrrolo [3, 4-c-]Pyridine replaces the methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.82(s，1H)，8.62(s，1H)，8.51(d，J＝5.0Hz，1H)，7.81-7.74(m，2H)，7.71-7.64(m，2H)，7.44(d，J＝5.1Hz，1H)，7.32(t，J＝5.8Hz，1H)，4.87-4.80(m，4H)，2.78-2.67(m，2H)，1.56(dp，J＝13.3，6.7Hz，1H)，1.30-1.13(m，2H)，0.78(d，J＝6.6Hz，6H)；MS(ESI(+))m/e389(M+H)+。
Example 883
N- (4- { [ (3-methoxybenzyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
N- (4-aminophenyl) isoindoline-2-carboxamide (0.0585g, 0.231mmol) was suspended in dichloromethane (2ml), followed by the addition of triisopropylethylamine (0.081ml, 0.462 mmol). (3-methoxyphenyl) methanesulfonyl chloride (0.061g, 0.277mmol) was dissolved in 1ml dichloromethane and slowly added to the mixture via syringe. The mixture was quenched with water and the separated aqueous layer was extracted with dichloromethane. The combined organic layers were dried over magnesium sulfate, filtered, and concentrated. Reverse phase HPLC was performed to provide the title compound.1H NMR(300MHz，DMSO-d6)δppm 8.65(s，1H)，8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.34(t，J＝5.6Hz，1H)，7.80-7.73(m，2H)，7.69-7.61(m，2H)，7.44(d，J＝5.0Hz，1H)，4.86-4.79(m，4H)，3.20(t，J＝6.2Hz，2H)，2.46-2.25(m，3H)，2.20(d，J＝7.9Hz，3H)，2.06-1.78(m，1H)，1.52-1.37(m，1H)；MS(ESI(+))m/e 438(M+H)+。
Example 909
N- {4- [6- (3-acetylphenyl) -4- (3-hydroxypropyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 909A
6-bromo-4- (3- (tert-butyldiphenylsiloxy) propyl) quinolin-2 (1H) -one
6-bromo-4- (3-hydroxypropyl) quinolin-2 (1H) -one (4.7g, 16.67mmole), imidazole (2.84g, 41.7mmole) and tert-butyldiphenylsilyl chloride (5.14ml, 20mmole) were stirred in dimethylformamide (60ml) at room temperature overnight. The reaction mixture was poured into water and extracted twice with ethyl acetate. The organic layers were combined, dried over magnesium sulfate, filtered, and concentrated. The crude product was purified by normal phase chromatography to afford the title compound.
Example 909B
4- (6-bromo-4- (3- (tert-butyldiphenylsiloxy) propyl) -2-oxoquinolin-1 (2H) -yl) butylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 797A substituting 6-bromo-4- (3- (tert-butyldiphenylsiloxy) propyl) quinolin-2 (1H) -one for 6-bromoquinolin-2 (1H) -one.
Example 909C
1- (4-Aminobutyl) -6-bromo-4- (3- (tert-butyldiphenylsiloxy) propyl) quinolin-2 (1H) -one
The title compound was prepared as described in example 2D substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (6-bromo-4- (3- (tert-butyldiphenylsiloxy) propyl) -2-oxoquinolin-1 (2H) -yl) butylcarbamate.
Example 909D
N- (4- (6-bromo-4- (3-hydroxypropyl) -2-oxoquinolin-1 (2H) -yl) butyl) isoindoline-2-carboxamide
The title compound was prepared as described in example 272B using 1- (4-aminobutyl) -6-bromo-4- (3- (tert-butyldiphenylsiloxy) propyl) quinolin-2 (1H) -one instead of 4-amino-N-propylbenzamide and isoindoline instead of methyl isoindoline-5-carboxylate hydrochloride, followed by TBAF deprotection and work-up.
Example 909E
N- {4- [6- (3-acetylphenyl) -4- (3-hydroxypropyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 280, substituting 3-acetylphenylboronic acid for 1H-pyrazol-3-ylboronic acid and N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide for 5-bromo-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1H NMR(400MHz，CDCl3)δppm 8.24(s，1H)，8.08(d，J＝2.0Hz，1H)，7.96(d，J＝7.9Hz，1H)，7.87-7.79(m，2H)，7.58(t，J＝7.7Hz，1H)，7.54(d，J＝8.8Hz，1H)，7.28(s，4H)，6.71(s，1H)，4.74(s，4H)，4.41(t，J＝7.4Hz，2H)，3.82(t，J＝6.0Hz，2H)，3.46(t，J＝6.7Hz，2H)，3.12-2.99(m，2H)，2.68(s，3H)，2.10-1.96(m，2H)，1.96-1.83(m，2H)，1.79-1.72(m，2H)；MS(APCI(+))m/e538(M+H)。
Example 910
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 910A
N- (4- (piperidin-4-yl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamides
In a 250mL Stainless Steel (SS) pressure bottle, N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide (2.0g, 6.24mmol) (in 80mL of 1: 1 THF: methanol) was added to 5% Pd/carbon (wet) (0.500g) and the mixture was stirred at 30atm and 25 ℃ for 38 hours. The mixture was filtered through a nylon membrane, concentrated, and suspended in ether. Filtration and washing with ether provided the title compound.
Example 910B
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, using N- (4- (piperidin-4-yl) phenyl) -1H-pyrrolo [3, 4-C ]]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and tetrahydrofuran-3-carboxylic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm 8.60(s，1H)，8.50(d，J＝5.0Hz，1H)，8.35(s，1H)，7.46(m，2H)，7.43(d，J＝5.0Hz，1H)，7.14(m，2H)，4.79(m，4H)，4.54(m，1H)，4.07(m，1H)，3.88(dt，J＝10.4，8.1Hz，1H)，3.71(m，3H)，3.37(m，1H)，3.13(m，1H)，2.64-2.59(m，2H)，2.01(m，2H)，1.79(m，2H)，1.46(m，2H)；MS(ESI(+))m/e 421(M+H)。
Table 15.
The following examples were prepared essentially as in example 1C, substituting N- (4- (piperidin-4-yl) phenyl) -1H-pyrrolo [3, 4-C ] pyridine-2 (3H) -carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 920
N- {5- [2- (2-chlorobenzyl) -1, 3-thiazol-4-yl ] -2-thienyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 920A
5- (2- (2-chlorobenzyl) thiazol-4-yl) thiophen-2-amine
The title compound was prepared as described in example 806A, substituting 2-bromo-1- (5-nitrothiophen-2-yl) ethanone for 2-bromo-1- (4-nitrophenyl) ethanone and 2- (2-chlorophenyl) thioacetamide for 2-phenylthioacetamide.
Example 920B
N- {5- [2- (2-chlorobenzyl) -1, 3-thiazol-4-yl ] -2-thienyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 5- (2- (2-chlorobenzyl) thiazol-4-yl) thiophen-2-amine for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. 1H NMR(400MHz，DMSO-d6，)δppm 9.73(s，1H)，7.46-7.55(m，3H)，7.34-7.40(m，4H)，7.28-7.34(m，2H)，7.20(d，J＝3.9Hz，1H)，6.62(d，J＝3.9Hz，1H)，4.76(s，4H)，4.45(s，2H)；MS(ESI(+))m/e 452.0(M+H)。
Example 921
N- [4- (4-fluorophenyl) butyl ] -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B substituting 4- (4-fluorophenyl) butylamine for 4-amino-N-propylbenzamide and isoindolin-5-ylmethanol hydrochloride for isoindoline-5-carboxylic acid methyl ester hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 7.28-7.17(m，5H)，7.13-7.03(m，2H)，6.29(t，J＝5.6Hz，1H)，5.16(t，J＝5.6Hz，1H)，4.54(bs，4H)，4.49(d，J＝5.5Hz，2H)，3.15-3.04(m，2H)，2.58(t，J＝7.4Hz，2H)，1.63-1.37(m，4H)；MS(ESI(+))m/e343(M+H)+。
Example 926
N- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
In a 20ml scintillation vial, N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c ] is added]Pyridine-2 (3H) -carboxamide (100mg, 0.312mmol), isobutyraldehyde (0.343mmol) and sodium triacetoxyborohydride (0.43mmol) were combined in dry dichloroethane (4 ml). The reaction mixture was stirred at room temperature overnight. By usingThe mixture was diluted with water and the resulting suspension was stirred again at room temperature overnight. The solid was filtered through a 30mL plastic disposable buchner funnel and the collected solid was washed with water, dried for 2 hours, washed with ether and dried again to provide the title compound.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ ppm8.58(s, 1H), 8.47(d, J ═ 5.0Hz, 1H), 8.18(m, 1H), 7.50(m, 2H), 7.38(d, J ═ 5.1Hz, 1H), 7.30(m, 2H), 6.03(m, 1H), 4.80(m, 4H), 3.06(m, 2H), 2.61(t, J ═ 5.6Hz, 2H), 2.44(m, 2H), 2.17(d, J ═ 7.2Hz, 2H), 1.82(m, 1H), 0.89(d, J ═ 6.6Hz, 6H); MS (ESI (+)) M/e 377(M + H).
Example 927
N- {4- [1- (tetrahydrofuran-3-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 926, substituting tetrahydrofuran-3-carbaldehyde for isobutyraldehyde.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ ppm 8.58(s, 1H), 8.48(d, J ═ 5.0Hz, 1H), 8.17(bs, 1H), 7.60(m, 2H), 7.38(d, J ═ 5.0Hz, 1H), 7.30(m, 2H), 6.05(m, 1H), 4.83(m, 4H), 3.77(m, 2H), 3.62(q, J ═ 7.6Hz, 1H), 3.39(m, 1H), 3.10(t, J ═ 3.1Hz, 2H), 2.95(m, 1H), 2.65(m, 2H), 2.43(m, 2H), 2.38(m, 2H), 1.95(m, 1H), 1.54(m, 1H); MS (ESI (+)) M/e 405(M + H).
Example 928
N- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 926, substituting tetrahydro-2H-pyran-4-carbaldehyde for isobutyraldehyde.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ ppm 8.58(s, 1H), 8.48(d, J ═ 5.0Hz, 1H), 8.17(bs, 1H), 7.50(m, 2H), 7.38(d, J ═ 5.1Hz, 1H), 7.30(m, 2H), 6.03(m, 1H), 4.79(m, 4H), 1.7)，3.83(m，2H)，3.31(td，J＝11.5，2.2Hz，2H)，3.07(m，2H)，2.63(t，J＝5.6Hz，2H)，2.43(m，2H)，2.27(d，J＝7.1Hz，2H)，1.80(m，1H)，1.64(m，2H)，1.17(m，2H)；MS(ESI(+))m/e 419(M+H)。
Example 929
N- [4- (1-isobutylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 926 using N- (4- (piperidin-4-yl) phenyl) -1H-pyrrolo [3, 4-c ]]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c)]Pyridine-2 (3H) -carboxamide.1H NMR(400MHz，DMSO-d6)δppm 8.60(s，1H)，8.50(d，J＝5.0Hz，1H)，8.33(s，1H)，7.43(m，3H)，7.13(m，2H)，4.79(m，4H)，2.41(m，1H)，2.92(m，2H)，2.15-1.85(m，4H)，1.85-1.50(m，5H)，0.87(d，J＝6.5Hz，6H)；MS(ESI(+))m/e 379(M+H)。
Example 930
N- {4- [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 926 using N- (4- (piperidin-4-yl) phenyl) -1H-pyrrolo [3, 4-c ]]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c)]Pyridine-2 (3H) -carboxamide, tetrahydrofuran-3-carboxaldehyde instead of isobutyraldehyde.1H NMR(400MHz，DMSO-d6)δppm 8.60(s，1H)，8.50(d，J＝5.0Hz，1H)，8.33(s，1H)，7.44(m，3H)，7.13(m，2H)，4.78(m，4H)，3.71(m，2H)，3.61(q，J＝7.6Hz，1H)，3.36(m，2H)，2.96(m，2H)，2.40(m，1H)，2.27(m，2H)，96(m，3H)，1.72(m，2H)，1.66-1.46(m，3H)；MS(ESI(+))m/e 407(M+H)。
Example 931
N- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 926 using N- (4- (piperidin-4-yl) phenyl) -1H-pyrrolo [3, 4-c ]]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) -1H-pyrrolo [3, 4-c)]Pyridine-2 (3H) -carboxamide, tetrahydro-2H-pyran-4-carbaldehyde substituted for isobutyraldehyde. 1H NMR(400MHz，DMSO-d6)δppm 8.60(s，1H)，8.49(d，J＝5.0Hz，1H)，8.33(s，1H)，7.44(m，3H)，7.12(m，2H)，4.79(m，4H)，3.83(m，2H)，3.27(m，2H)，2.92(m，2H)，2.40(m，1H)，2.14(d，J＝7.2Hz，2H)，1.95(m，2H)，1.74(m，3H)，1.61(m，4H)，1.12(m，2H)；MS(ESI(+))m/e 421(M+H)。
Example 933
{4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzyl } carbamic acid tert-butyl ester
The title compound was prepared as described in example 272B substituting 4-aminobenzylcarbamic acid tert-butyl ester for 4-amino-N-propylbenzamide and isoindoline for isoindoline-5-carboxylic acid methyl ester hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.29(s，1H)，7.52-7.45(m，2H)，7.40-7.24(m，5H)，7.15-7.08(m，2H)，4.76(bs，4H)，4.09-3.99(m，2H)，1.39(s，9H)；MS(ESI(+))m/e 368(M+H)+。
Example 934
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 934A
N- (4-Nitrophenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamides
The title compound was prepared as described in example 1A, substituting 1-isocyanato-4-nitrobenzene for methyl 4-isocyanatobenzoate and 1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine for isoindoline.
Example 934B
N- (4-aminophenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 272A, substituting N- (4-nitrophenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide for 4-nitro-N-propylbenzamide.
Example 934C
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, using N- (4-aminophenyl) -1H-pyrrolo [3, 4-C ] ]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and cyclopentylacetic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 9.70(s，1H)，8.60(s，1H)，8.50(d，J＝5.0Hz，1H)，8.34(s，1H)，7.51-7.40(m，5H)，4.82-4.75(m，4H)，2.33-2.17(m，3H)，1.81-1.68(m，2H)，1.68-1.43(m，4H)，1.27-1.13(m，2H)；(ESI(+))m/e365(M+H)+。
Example 936
N- [4- (5- { [ (tetrahydrofuran-2-ylmethyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 753B, substituting (tetrahydrofuran-2-yl) methylamine for morpholine.1H NMR(300MHz，DMSO-d6)δppm 8.68(s，1H)，7.91(d，J＝8.7Hz，2H)，7.79(d，J＝8.8Hz，2H)，7.45-7.20(m，4H)，4.80(s，4H)，4.08(s，2H)，3.95-3.78(m，1H)，3.79-3.66(m，1H)，3.66-3.49(m，1H)，2.66(d，J＝5.6Hz，2H)，2.00-1.67(m，4H)，1.67-1.41(m，2H)，1.40-1.16(m，2H)，0.87(dd，J＝9.3，5.4Hz，1H)；MS(ESI(+))m/e420(M+H)+。
Example 937
N- (4- {5- [ (4-methoxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 753B, substituting morpholine with 4-methoxypiperidine.1H NMR(300MHz，DMSO-d6)δppm 8.69(s，1H)，7.92(d，J＝8.8Hz，2H)，7.80(d，J＝8.8Hz，2H)，7.45-7.20(m，4H)，4.80(s，4H)，3.93(s，2H)，3.21(s，3H)，3.20-3.10(m，1H)，2.82-2.68(m，2H)，2.50(dt，J＝3.6，1.8Hz，2H)，2.41-2.24(m，2H)，1.92-1.75(m，2H)，1.56-1.37(m，2H)；MS(ESI(+))m/e 434(M+H)+。
Example 938
N- [4- (5- { [4- (2-methoxyethyl) piperazin-1-yl ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 753B, substituting N- (2-methoxyethyl) piperazine for morpholine.1H NMR(300MHz，DMSO-d6)δppm 8.69(s，1H)，7.92(d，J＝8.8Hz，2H)，7.86-7.70(m，2H)，7.46-7.23(m，4H)，4.80(s，4H)，3.93(s，2H)，3.40(t，J＝5.8Hz，3H)，3.21(s，3H)，2.55(s，4H)，2.45(t，J＝5.8Hz，6H)；MS(ESI(+))m/e 463(M+H)+。
Example 940
N- {4- [ (1-pentanoylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 940A
4- (4-Nitrophenoxy) piperidine-1-carboxylic acid tert-butyl ester
Tert-butyl 4-hydroxy-1-piperidine-1-carboxylate (6.04g, 30mmol) was dissolved in 1-fluoro-4-nitrobenzene (7.83g, 55.5 mmol). Aqueous potassium hydroxide (25 wt%, 44ml) was added followed by tetrabutylammonium bromide (1.26 g). The reaction mixture was stirred at 35 ℃ for 17 hours. The solid was collected by filtration, washed with water (4 × 50mL) and dried under vacuum to provide the title compound.
Example 940B
4- (4-Aminophenoxy) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 274, substituting 4- (4-nitrophenoxy) piperidine-1-carboxylic acid tert-butyl ester for 5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxamide.
Example 940C
4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenoxy) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272B substituting 4- (4-aminophenoxy) piperidine-1-carboxylic acid tert-butyl ester for 4-amino-N-propylbenzamide and 1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine for isoindoline-5-carboxylic acid methyl ester hydrochloride.
Example 940D
N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 2D, substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenoxy) piperidine-1-carboxylate.
Example 940E
N- {4- [ (1-pentanoylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-C]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and pentanoic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.80(s，1H)，8.68(d，J＝5.5Hz，1H)，8.36(s，1H)，7.77(d，J＝5.5Hz，1H)，7.42(d，J＝9.0Hz，1H)，6.95-6.87(m，2H)，4.87(d，J＝6.4Hz，4H)，4.64-4.45(m，1H)，3.92-3.79(m，1H)，3.76-3.63(m，1H)，3.38-3.15(m，2H)，2.31(t，J＝7.4Hz，2H)，1.96-1.81(m，2H)，1.61-1.41(m，4H)，1.38-1.22(m，2H)，0.88(t，J＝7.2Hz，3H)；MS(ESI(+))m/e 423(M+H)+。
Table 16.
The following examples are prepared essentially as in example 940, substituting the appropriate alcohol for tert-butyl 4-hydroxy-1-piperidine-1-carboxylate in example 940A and the appropriate carboxylic acid in example 940E.
Example 953
N- {6- [ (1-acetylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 953A
4- (5-Nitropyridin-2-yloxy) piperidine-1-carboxylic acid tert-butyl ester
A suspension of previously washed NaH (0.1g, 2.48mmol, 60% dispersion in mineral oil) in THF (2ml) was added to an ice-cold solution of 4-hydroxy-piperidine-1-carboxylic acid tert-butyl ester (0.5g, 2.48mmol) in dry THF (3 ml). The mixture was stirred for 20 min and added in portions to 2-chloro-5-nitro-pyridine (0.36g, 2.26 mmol). After the addition was complete, the cooling bath was removed and the reaction mixture was stirred at 22 ℃ overnight. The reaction mixture was cooled in an ice bath and treated with saturated aqueous sodium bicarbonate (5 mL). The reaction mixture was diluted with ethyl acetate (25mL) and distilled water (25 mL). The separated aqueous phase was extracted with ethyl acetate (3 × 35mL) and the combined organic phases were dried over sodium sulfate, filtered and concentrated under reduced pressure. Chromatography was performed to provide the title compound.
Example 953B
4- (5-Aminopyridin-2-yloxy) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 274, substituting 4- (5-nitropyridin-2-yloxy) piperidine-1-carboxylic acid tert-butyl ester for 5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxamide.
Example 953C
4- (5- (isoindoline-2-carboxamido) pyridin-2-yloxy) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272B with 4- (5-aminopyridin-2-yloxy) piperidine-1-carboxylic acid tert-butyl ester instead of 4-amino-N-propylbenzamide and isoindoline instead of isoindoline-5-carboxylic acid methyl ester hydrochloride.
Example 953D
N- (6- (piperidin-4-yloxy) pyridin-3-yl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D, substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (5- (isoindoline-2-carboxamido) pyridin-2-yloxy) piperidine-1-carboxylate.
Example 953E
N- {6- [ (1-acetylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (6- (piperidin-4-yloxy) pyridin-3-yl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and acetic acid for 4- (isoindoline-2-carboxamido) benzoic acid. 1H NMR(300MHz，DMSO-d6)δppm8.37(s，1H)，8.26(d，J＝2.7Hz，1H)，7.86(dd，J＝8.9，2.7Hz，1H)，7.44-7.24(m，4H)，6.75(d，J＝8.8Hz，1H)，5.21-5.07(m，1H)，4.75(s，4H)，3.72-3.63(m，1H)，3.40-3.11(m，2H)，1.97-1.85(m，1H)，1.73-1.38(m，2H)；MS(ESI(+))m/e 495(M+H)+。
Table 17.
The following examples were prepared essentially as described in example 1C, substituting N- (6- (piperidin-4-yloxy) pyridin-3-yl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the appropriate formic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 966
(2- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } ethyl) carbamic acid tert-butyl ester
The title compound was prepared as described in example 272B substituting tert-butyl 4-aminophenylethylcarbamate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.26(s，1H)，7.50-7.43(m，2H)，7.40-7.26(m，4H)，7.11-7.03(m，2H)，6.87-6.79(m，1H)，4.75(s，4H)，3.18-3.02(m，2H)，2.66-2.58(m，2H)，1.37(s，9H)；MS(ESI(+))m/e 382(M+H)+。
Example 973
N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 808, substituting (tetrahydrofuran-3-yl) methylamine for 3-methylbutan-1-amine in example 808A.1H NMR(300MHz，DMSO-d6)δppm 8.76(s，1H)，7.82-7.75(m，2H)，7.71-7.64(m，2H)，7.54(t，J＝6.1Hz，1H)，7.41-7.25(m，4H)，4.80(bs，4H)，3.70-3.49(m，3H)，2.69(t，J＝6.7Hz，2H)，2.34-2.16(m，1H)，1.94-1.79(m，1H)，1.54-1.39(m，1H)；MS(ESI(+))m/e 402(M+H)+。
Example 974
N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 272B, substituting 4-amino-N- ((tetrahydrofuran-3-yl) methyl) benzenesulfonamide for 4-amino-N-propylbenzamide, 1, 3-dihydro-2H-pyrrolo [3, 4-c) ]Pyridine replaces the methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.83(s，1H)，8.62(s，1H)，8.51(d，J＝5.0Hz，1H)，7.82-7.75(m，2H)，7.72-7.65(m，2H)，7.55(t，J＝6.0Hz，1H)，7.44(d，J＝5.1Hz，1H)，4.87-4.75(m，4H)，3.76-3.49(m，3H)，2.69(t，J＝6.7Hz，2H)，2.34-2.16(m，1H)，1.94-1.79(m，1H)，1.54-1.39(m，1H)；MS(ESI(+))m/e 403(M+H)+。
Example 975
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B using 4-amino-N- ((tetrahydrofuran-3-yl) methyl) benzenesulfonamide instead of 4-amino-N-propylbenzamide and isoindoline-5-carbonitrile instead of methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.83(s，1H)，7.89(s，1H)，7.83-7.74(m，3H)，7.72-7.64(m，2H)，7.59(d，J＝7.9Hz，1H)，7.54(t，J＝6.1Hz，1H)，4.93-4.76(m，4H)，3.70-3.49(m，3H)，2.69(t，J＝6.7Hz，2H)，2.31-2.05(m，1H)，1.94-1.78(m，1H)，1.54-1.39(m，1H)；MS(ESI(+))m/e 427(M+H)+。
Example 979
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 979A
N- (4- (piperidin-4-yl) phenyl) isoindoline-2-carboxylic acid amide
In a 50ml pressure bottle, tert-butyl 4- (4- (isoindoline-2-carboxamido) phenyl) -5, 6-dihydropyridine-1 (2H) -carboxylate (1.00g, 2.38mmol) in 20ml of 1: 1 methanol/tetrahydrofuran was added to 5% Pd/carbon (wet) (0.200g) and stirred at 30atm at room temperature for 16 hours. The mixture was filtered through a nylon membrane and concentrated. The residue was suspended in dichloromethane, stirred for 1 hour, filtered and washed with dichloromethane to provide the title compound.
Example 979B
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (piperidin-4-yl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and tetrahydrofuran-3-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm8.26(s，1H)，7.46(m，2H)，7.31(m，4H)，7.12(m，2H)，4.74(bs，4H)，4.53(m，1H)，4.05(m，1H)，3.87(m，1H)，3.70(m，3H)，3.36(m，2H)，3.12(m，1H)，2.75-2.58(m，1H)，2.01(m，2H)，1.76(m，2H)，1.45(m，2H)；MS(ESI(+))m/e 420(M+H)。
Table 18.
The following examples were prepared essentially as described in example 1C, substituting the appropriate amine for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 1013
N- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 1013A
4- (4- (isoindoline-2-carboxamido) phenoxy) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272B substituting 4- (4-aminophenoxy) piperidine-1-carboxylic acid tert-butyl ester for 4-amino-N-propylbenzamide and isoindoline for isoindoline-5-carboxylic acid methyl ester hydrochloride.
Example 1013B
N- (4- (piperidin-4-yloxy) phenyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D substituting 4- (4- (isoindoline-2-carboxamido) phenoxy) piperidine-1-carboxylic acid tert-butyl ester for 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.
Example 1013C
N- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (piperidin-4-yloxy) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and tetrahydrofuran-3-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.20(s，1H)，7.47-7.27(m，6H)，6.93-6.86(m，2H)，4.74(s，4H)，4.58-4.47(m，1H)，3.93-3.56(m，6H)，3.44-3.32(m，3H)，2.06-1.83(m，4H)，1.69-1.40(m，2H)；MS(ESI(+))m/e 436(M+H)+。
Table 19.
The following examples were prepared essentially as described in example 1C, substituting the appropriate amine for 3-phenylpropan-1-amine and the appropriate acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 1018
N- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1018A
N- (4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine 2. HCl (1.55g, 8.03mmol) was suspended in dimethylformamide (30ml) and treated with triisopropylethylamine (4.21ml, 24.08 mmol). After stirring for 20 minutes, the mixture was cooled to-15 ℃. 2- (4-isocyanatophenyl) -4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolane (2.028g, 8.03mmol) was dissolved in 10ml of tetrahydrofuran and added via syringe over 10 minutes. The mixture was warmed to room temperature, stirred for 3 hours, and concentrated to a minimum volume under a stream of nitrogen. The residue was diluted with cold water to give a cloudy mixture which was filtered, washed with water and dried to provide the title compound.
Example 1018B
4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) cyclohex-3-enylcarbamic acid tert-butyl ester
Reacting N- (4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) phenyl) -1H-pyrrolo [3, 4-c)]Pyridine-2 (3H) -carboxamide (1.692g, 4.63mmol), 4- (tert-butoxycarbonylamino) cyclohex-1-enyl triflate (1.6g, 4.63mmol) and cesium carbonate (3.77g, 11.58mmol) were suspended in tetrahydrofuran (30ml), methanol (5.00ml) and water (15.00 ml). When PdCl is added2(dppf) -dichloromethane adduct (0.189g, 0.232mmol), nitrogen was bubbled through the solution for 10 minutes, and the mixture was heated to 80 ℃ for 7 hours. After dilution with ethyl acetate and brine, the separated aqueous layer was extracted several times with ethyl acetate, and the combined organic layers were dried over magnesium sulfate, filtered, and concentrated. Flash chromatography was performed to provide the title compound.
Example 1018C
N- (4- (4-aminocyclohex-1-enyl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 2D substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) cyclohex-3-enylcarbamate.
Example 1018D
N- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohex-1-enyl) phenyl) -1H-pyrrolo [3, 4-C)]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and isobutyric acid instead of 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.41(s，1H)，7.66(d，J＝7.6Hz，1H)，7.56-7.48(m，2H)，7.43(d，J＝5.1Hz，1H)，7.37-7.29(m，2H)，6.06-5.99(m，1H)，4.83-4.77(m，4H)，3.87-3.73(m，1H)，2.37(t，J＝6.7Hz，2H)，2.11-1.97(m，1H)，1.95-1.82(m，1H)，1.80-1.50(m，1H)，1.38-1.20(m，2H)，1.00(dd，J＝6.8，2.5Hz，6H)；MS(ESI(+))m/e 405(M+H)+。
Table 20.
The title compound was prepared as described in example 1C, substituting N- (4- (4-aminocyclohex-1-enyl) phenyl) -1H-pyrrolo [3, 4-C ] pyridine-2 (3H) -carboxamide for 3-phenylprop-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 1020
3- { [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] methyl } azetidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272B, substituting 3- (aminomethyl) azetidine-1-carboxylic acid tert-butyl ester for 4-amino-N-propylbenzamide and isoindoline for isoindoline-5-carboxylic acid methyl ester hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 7.37-7.23(m，4H)，6.58-6.48(m，1H)，4.58(s，4H)，3.91-3.75(m，2H)，3.65-3.51(m，2H)，3.30-3.20(m，2H)，2.68-2.55(m，1H)，1.35(s，9H)；MS(ESI(+))m/e 332(M+H)+。
Example 1021
[ (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } azetidin-3-yl) methyl ] carbamic acid tert-butyl ester
Example 1021A
(1- (4-Nitrophenyl) azetidin-3-yl) methylcarbamic acid tert-butyl ester
A solution of 1-fluoro-4-nitrobenzene (0.61g, 4.32mmol) and tert-butyl azetidin-3-ylmethylcarbamate (0.886g, 4.76mmol) in dimethylformamide (8.65ml) was treated with potassium carbonate (0.896g, 6.48mmol) and the suspension was heated at 55 deg.C (12pm) for 3 h and at ambient temperature for 16 h. The reaction was poured into water and the suspension was filtered. The solid was washed with water and dried to provide the title compound.
Example 1021B
(1- (4-aminophenyl) azetidin-3-yl) methylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 272A, substituting tert-butyl (1- (4-nitrophenyl) azetidin-3-yl) methylcarbamate for 4-nitro-N-propylbenzamide.
Example 1021C
[ (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } azetidin-3-yl) methyl ] carbamic acid tert-butyl ester
The title compound was prepared as described in example 272B substituting tert-butyl (1- (4-aminophenyl) azetidin-3-yl) methylcarbamate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. 1H NMR(300MHz，DMSO-d6)δppm 8.03(s，1H)，7.39-7.25(m，6H)，7.07-6.94(m，1H)，6.33(d，J＝8.8Hz，2H)，4.72(s，4H)，3.75(t，J＝7.4Hz，2H)，3.48-3.40(m，2H)，3.22-3.14(m，2H)，2.76-2.65(m，1H)，1.38(s，9H)；MS(ESI(+))m/e 423(M+H)+。
Example 1046
N- [4- ({ [4- (acetylamino) phenyl ] sulfonyl } amino) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, 4- (acetylamino) phenyl]Sulfonyl chloride was substituted for (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.72(s, 1H)8.62(d, J ═ 4.88Hz, 1H)7.73(d, J ═ 5.49Hz, 1H)7.61-7.69(m, 4H)7.36(d, J ═ 8.54Hz, 2H)6.98(d, J ═ 8.85Hz, 2H)4.88(d, J ═ 7.02Hz, 4H)2.00-2.10(m, 3H); MS (APCI (+)) M/e 452(M + H)+。
Example 1047
N- {4- [ (propylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, propanesulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1H NMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.72(s, 1H)8.62(d, J ═ 5.49Hz, 1H)7.73(d, J ═ 5.49Hz, 1H)7.46(d, J ═ 8.54Hz, 2H)7.14(d, J ═ 8.85Hz, 2H)4.91(d, J ═ 6.10Hz, 4H)2.98-3.06(m, 2H)1.66-1.78(m, 2H)0.96(t, J ═ 7.48Hz, 3H); MS (APCI (+)) M/e 361(M + H) +。
Example 1048
N- (4- { [ (4-propylphenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, (4-propylphenyl) sulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1H NMR(300MHz，DMSO-d6)δ9.90(s，1H)，8.59(s，1H)，8.49(d，J＝5.0Hz，1H)，8.33(s，1H)，7.64-7.58(m，2H)，7.45-7.33(m，4H)，7.33(s，1H)，6.99-6.92(m，2H)，4.79-4.72(m，4H)，2.57(dd，J＝17.1，9.3Hz，1H)，1.65-1.49(m，2H)，0.86(t，J＝7.3Hz，3H)；MS(ESI(+))m/e437(M+H)+。
Example 1049
N- {4- [ (butanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide and butanesulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1H NMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.71(s, 1H)8.61(d, J ═ 5.19Hz, 1H)7.70(d, J ═ 5.49Hz, 1H)7.47(d, J ═ 8.85Hz, 2H)7.14(d, J ═ 8.85Hz, 2H)4.90(d, J ═ 3.66Hz, 4H)2.97-3.08(m, 2H)1.61-1.72(m, 2H)1.30-1.44(m, 2H)0.85(t, J ═ 7.32Hz, 3H); MS (APCI (+)) M/e375(M + H)+。
Example 1050
N- {4- [ ({ [ (1S, 4R) -7, 7-dimethyl-2-oxobicyclo [2.2.1] hept-1-yl ] methyl } sulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Substitution of pyridine-2 (3H) -carboxamide for N- (4-aminophenyl) isoindoline-2-carboxamide, (1S, 4R) -7, 7-dimethyl-2-oxobicyclo [ 2 ], [2.2.1]Hept-1-yl]Methyl } sulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1H NMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.72(s, 1H)8.61(d, J ═ 5.19Hz, 1H)7.71(d, J ═ 5.49Hz, 1H)7.49(d, J ═ 8.85Hz, 2H)7.18(d, J ═ 8.85Hz, 2H)4.90(d, J ═ 3.97Hz, 4H)2.81(s, 2H)2.27-2.41(m, 2H)2.07(t, J ═ 4.43Hz, 1H)1.94-2.03(m, 2H)1.34-1.66(m, 2H)1.02(s, 3H)0.79(s, 3H); MS (APCI (+)) M/e469(M + H)+。
Example 1051
N- {4- [ (ethylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, ethanesulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1H NMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.70-8.75(m, 1H)8.60-8.64(m, J-5.65, 5.65Hz, 1H)7.74(d, J-5.19 Hz, 1H)7.46(d, J-8.85 Hz, 2H)7.15(d, J-8.54 Hz, 2H)4.91(d, J-7.02 Hz, 4H)3.04(q, J-7.32 Hz, 2H)1.23(t, J-7.32 Hz, 3H); MS (APCI (+)) M/e 347(M + H) +。
Example 1052
N- {4- [ (benzylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, benzylsulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1H NMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.72(s, 1H)8.61(d, J ═ 4.88Hz, 1H)7.70(d, J ═ 5.19Hz, 1H)7.46(d, J ═ 8.85Hz, 2H)7.28-7.37(m, 5H)7.11(d, J ═ 8.85Hz, 2H)4.90(d, J ═ 3.05Hz, 4H)4.37(s, 2H); MS (APCI (+)) M/e 409(M + H)+。
Example 1053
N- (4- { [ (4-fluorophenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, (4-fluorophenyl) sulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1H NMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.71(s, 1H)8.61(d, J ═ 5.19Hz, 1H)7.78(dd, J ═ 8.85, 5.19Hz, 2H)7.67-7.73(m, 1H)7.28-7.43(m, 4H)6.98(d, J ═ 8.85Hz, 2H)4.87(d, J ═ 4.27Hz, 4H); MS (APCI (+)) M/e412(M + H) +。
Example 1054
N- {4- [ (thiophen-2-ylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4-aminophenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide and thiophen-2-ylsulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1H NMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.70(s, 1H)8.61(d, J ═ 4.88Hz, 1H)7.81(d, J ═ 4.88Hz, 1H)7.69(d, J ═ 5.19Hz, 1H)7.49(d, J ═ 2.75Hz, 1H)7.42(d, J ═ 8.85Hz, 2H)7.09-7.13(m, 1H)7.04(d, J ═ 8.85Hz, 2H)4.88(d, J ═ 3.36Hz, 4H); MS (APCI (+)) M/e 401(M + H)+。
Example 1088
N- [4- (piperidin-1-ylsulfonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 272B, substituting 4- (piperidin-1-ylsulfonyl) aniline for 4-amino-N-propylbenzamide, 1, 3-dihydro-2H-pyrrolo [3, 4-c)]Pyridine substituted isoindolines-5-carboxylic acid methyl ester hydrochloride.1H NMR(300MHz，DMSO-d6)δppm8.89(s，1H)，8.62(s，1H)，8.51(d，J＝5.0Hz，1H)，7.86-7.79(m，2H)，7.66-7.59(m，2H)，7.44(d，J＝5.0Hz，1H)，4.89-4.76(m，4H)，3.25-3.00(m，1H)，2.95-2.82(m，4H)，1.57-1.44(m，4H)，1.41-1.31(m，1H)；MS(ESI(+))m/e 387(M+H)+。
Example 1246
1- {4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } azetidine-3-carboxylic acid methyl ester
Example 1246A
1- (4-Nitrophenyl) azetidine-3-carboxylic acid methyl ester
Azetidine-3-carboxylic acid methyl ester hydrochloride (1.236g, 8.15mmol) and N-methylmorpholine (2.338ml, 21.26mmol) in dimethylformamide (10ml) and 1-fluoro-4-nitrobenzene (1g, 7.09mmol) in dimethylformamide (7ml) were treated and the reaction stirred at room temperature for 60 h. Water (50ml) was added and the resulting suspension was stirred for 10 min and filtered. The collected solid was washed with water and dried in vacuo. Flash chromatography of the collected solid afforded the title compound.
Example 1246B
1- (4-aminophenyl) azetidine-3-carboxylic acid methyl ester
The title compound was prepared as described in example 272A, substituting 1- (4-nitrophenyl) azetidine-3-carboxylic acid methyl ester for 4-nitro-N-propylbenzamide.
Example 1246C
1- {4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } azetidine-3-carboxylic acid methyl ester
The title compound was prepared as described in example 272B, substituting 1- (4-aminophenyl) azetidine-3-carboxylic acid methyl ester for 4-amino-N-propylbenzamide, 1, 3-bishydro-2H-pyrrolo [3, 4-c]Pyridine replaces the methyl isoindoline-5-carboxylate hydrochloride. 1H NMR(300MHz，DMSO-d6)δppm 8.60(s，1H)，8.49(d，J＝5.0Hz，1H)，8.15(s，1H)，7.42(d，J＝5.1Hz，1H)，7.36-7.29(m，2H)，6.44-6.37(m，2H)，4.80-4.72(m，4H)，4.02-3.93(m，2H)，3.86-3.77(m，2H)，3.68(s，3H)，3.66-3.56(m，1H)；MS(ESI(+))m/e 353(M+H)+。
Example 1247
N- (4- {3- [ (3-methylbutyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1247A
1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) azetidine-3-carboxylic acid
The title compound was prepared as described in example 1B substituting methyl 1- {4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } azetidine-3-carboxylate for methyl 4- (isoindoline-2-carboxamido) benzoate.
Example 1247B
N- (4- {3- [ (3-methylbutyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-carboxamido) phenyl) azetidine-3-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1HNMR(300MHz，DMSO-d6)δppm 8.59(s，1H)，8.49(d，J＝5.0Hz，1H)，8.13(s，1H)，7.90(t，J＝5.5Hz，1H)，7.42(d，J＝4.8Hz，1H)，7.34-7.27(m，2H)，6.41-6.34(m，2H)，4.79-4.73(m，4H)，3.94-3.85(m，2H)，3.76-3.69(m，2H)，3.47-3.36(m，1H)，3.13-3.04(m，2H)，1.65-1.48(m，1H)，1.35-1.24(m，2H)，0.87(d，J＝6.6Hz，6H)；MS(ESI(+))m/e 408(M+H)+。
Example 1248
N- (4- {3- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting (tetrahydrofuran-2-yl) methylamine for 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-C) ]Pyridine-2-carboxamido) phenyl) azetidine-3-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1HNMR(300MHz，DMSO-d6)δppm 8.59(s，1H)，8.49(d，J＝5.0Hz，1H)，8.13(s，1H)，8.05(t，J＝5.8Hz，1H)，7.42(d，J＝5.1Hz，1H)，7.35-7.27(m，2H)，6.41-6.34(m，2H)，4.79-4.73(m，4H)，3.94-3.68(m，6H)，3.68-3.55(m，1H)，3.54-3.39(m，1H)，3.20-3.07(m，2H)，1.93-1.71(m，3H)，1.55-1.41(m，1H)；MS(ESI(+))m/e 422(M+H)+。
Example 1249
N- (4- {3- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting (tetrahydro-2H-pyran-4-yl) methylamine for 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-carboxamido) phenyl) azetidine-3-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.59(s，1H)，8.49(d，J＝5.0Hz，1H)，8.13(s，1H)，7.97(t，J＝5.8Hz，1H)，7.42(d，J＝5.1Hz，1H)，7.34-7.27(m，2H)，6.41-6.34(m，2H)，4.79-4.73(m，4H)，3.95-3.86(m，2H)，3.86-3.78(m，2H)，3.77-3.69(m，2H)，3.51-3.40(m，1H)，3.31-3.19(m，2H)，3.02-2.94(m，2H)，1.69-1.48(m，3H)，1.22-1.04(m，2H)；MS(ESI(+))m/e 436(M+H)+。
Example 1250
N- {4- [3- (benzylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C substituting benzylamine for 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-carboxamido) phenyl) azetidine-3-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.59(s，1H)，8.53-8.45(m，2H)，8.13(s，1H)，7.42(d，J＝5.0Hz，1H)，7.37-7.22(m，7H)，6.43-6.35(m，2H)，4.76(m，4H)，4.30(d，J＝5.9Hz，2H)，3.99-3.88(m，2H)，3.83-3.72(m，2H)，3.57-3.46(m，1H)；MS(ESI(+))m/e 428(M+H)+。
Example 1251
N- {4- [3- (cyclopentylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C substituting cyclopentylamine for 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-C) ]Pyridine-2-carboxamido) phenyl) azetidine-3-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.59(s，1H)，8.49(d，J＝5.0Hz，1H)，8.13(s，1H)，7.91(d，J＝7.2Hz，1H)，7.42(d，J＝5.1Hz，1H)，7.34-7.27(m，2H)，6.41-6.33(m，2H)，4.79-4.73(m，4H)，4.06-3.94(m，1H)，3.92-3.84(m，2H)，3.76-3.66(m，2H)，3.46-3.33(m，1H)，1.86-1.72(m，2H)，1.67-1.30(m，6H)；MS(ESI(+))m/e 406(M+H)+。
Example 1252
N- (4- {3- [ (cyclopentylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1CIn which cyclopentylmethylamine is used to replace 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c)]Pyridine-2-carboxamido) phenyl) azetidine-3-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.59(s，1H)，8.49(d，J＝5.0Hz，1H)，8.13(s，1H)，7.96(t，J＝5.7Hz，1H)，7.42(d，J＝4.7Hz，1H)，7.34-7.27(m，2H)，6.41-6.33(m，2H)，4.81-4.72(m，4H)，3.94-3.85(m，2H)，3.77-3.68(m，2H)，3.50-3.37(m，1H)，3.04-2.97(m，2H)，2.04-1.89(m，1H)，1.71-1.39(m，6H)，1.25-1.08(m，2H)；MS(ESI(+))m/e420(M+H)+。
Example 1253
N- (4- {3- [ (2-methoxyethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C substituting 2-methoxyethyl-1-ylamine for 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-carboxamido) phenyl) azetidine-3-carboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1HNMR(300MHz，DMSO-d6)δppm 8.59(s，1H)，8.49(d，J＝5.0Hz，1H)，8.13(s，1H)，8.05(t，J＝5.5Hz，1H)，7.42(d，J＝5.1Hz，1H)，7.35-7.27(m，2H)，6.42-6.34(m，2H)，4.79-4.73(m，4H)，3.93-3.86(m，2H)，3.73(t，J＝6.6Hz，2H)，3.52-3.41(m，1H)，3.38-3.30(m，2H)，3.27-3.21(m，5H)；MS(ESI(+))m/e 396(M+H)+。
Example 1268
N- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting (S) - (tetrahydrofuran-2-yl) methylamine for 3-phenylprop-1-amine, and 6- (isoindoline-2-carboxamido) pyridazine-3-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid. 1H NMR(300MHz，DMSO-d6)δ10.03(s，1H)，8.85(t，J＝6.1Hz，1H)，8.32(d，J＝9.3Hz，1H)，8.12(d，J＝9.3Hz，1H)，7.41-7.28(m，4H)，5.04-4.72(m，4H)，4.04(p，J＝6.2Hz，1H)，3.85-3.74(m，1H)，3.69-3.58(m，1H)，3.38(dd，J＝11.2，5.0Hz，2H)，2.01-1.74(m，3H)，1.71-1.54(m，1H)；MS(ESI(+))m/e368(M+H)+。
Example 1285
N- {4- [ (4-fluorobenzyl) (3-methylbutyryl) amino ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 1285A
4- (4-Fluorobenzylamino) butylcarbamic acid tert-butyl ester
Tert-butyl 4-bromobutylcarbamate (0.735g, 2.91mmole), (4-fluorophenyl) methylamine (0.333g, 2.91mmole) and potassium carbonate (0.806g, 5.83mmole) were stirred in acetonitrile (15ml) at 100 ℃ for 1 hour. The reaction mixture was cooled, the solvent was concentrated, and the residue was taken up in dichloromethane and washed twice with water. The organic layers were combined, dried over magnesium sulfate, filtered, and concentrated to provide the title compound, which was used in the next step without further purification.
Example 1285B
4- (N- (4-fluorobenzyl) -3-methylbutyrylamino) butylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 278, substituting 3-methylbutanoyl chloride for acetyl chloride, and tert-butyl 4- (4-fluorobenzylamino) butylcarbamate for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.
Example 1285C
N- (4-aminobutyl) -N- (4-fluorobenzyl) -3-methylbutanamide
The title compound was prepared as described in example 2D substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (N- (4-fluorobenzyl) -3-methylbutyrylamino) butylcarbamate.
Example 1285D
N- {4- [ (4-fluorobenzyl) (3-methylbutyryl) amino ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 272B using N- (4-aminobutyl) -N- (4-fluorobenzyl) -3-methylbutanamide in place of 4-amino-N-propylbenzamide and isoindoline in place of methyl isoindoline-5-carboxylate hydrochloride.1H NMR(400MHz，CDCl3)δppm 7.34-7.27(m，4H)，7.23(dd，J＝8.5，5.5Hz，1H)，7.13(dd，J＝8.5，5.5Hz，1H)，7.06(t，J＝8.6Hz，1H)，6.99(t，J＝8.6Hz，1H)，5.49-5.17(m，1H)，4.72(m，4H)，4.56(d，J＝17.7Hz，2H)，3.34(m，4H)，2.29(m，2H)，2.23-2.12(m，1H)，1.68-1.50(m，4H)，1.01-0.93(d，J＝6.9Hz，6H)；MS(APCI(+))m/e 426(M+H)+。
Example 1286
N- [4- (9-chloro-5-oxo-2, 3, 3a, 4, 4a, 5-hexahydro-6H-furo [2 ', 3': 2, 3] cyclobuta [1, 2-c ] quinolin-6-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1286A
4- (but-3-enyloxy) -6-chloroquinolin-2 (1H) -one
To a solution of 6-chloro-4-hydroxyquinolin-2 (1H) -one (800mg, 4.09mmol) and N, N-diisopropylethylamine (1415. mu.l, 8.18mmol) in dimethylformamide (13.6ml) was added 4-bromo-1-butene (415. mu.l, 4.09 mmol). The solution was heated to 60 ℃ and stirred for 18 hours. The reaction mixture was purified by column chromatography to provide the title compound.
Example 1286B
9-chloro-3, 3a, 4, 4 a-tetrahydro-2H-furo [2 ', 3': 2, 3] cyclobuta [1, 2-c ] quinolin-5 (6H) -one
A solution of 4- (but-3-enyloxy) -6-chloroquinolin-2 (1H) -one (600mg, 2.403mmol) in benzene (240ml) was placed under a 450W Hg UV lamp (equipped with a condenser for cooling) and stirred for 4 days (96H). The mixture was then cooled, concentrated in vacuo, and taken up in-75 mL of dichloromethane (slightly heated to dissolve as much as possible). The sample (which is a mixture of regioisomers) was purified by column chromatography. The second eluted compound was concentrated to provide the title compound.
Example 1286C
Tert-butyl [4- (9-chloro-5-oxo-2, 3, 3a, 4, 4a, 5-hexahydro-6H-furo [2 ', 3': 2, 3] cyclobut (cyclobuta) [1, 2-c ] quinolin-6-yl) butyl ] carbamate
To a solution of 9-chloro-3, 3a, 4, 4 a-tetrahydro-2H-furo [2 ', 3': 2, 3] cyclobuta [1, 2-c ] quinolin-5 (6H) -one (200mg, 0.801mmol) in dimethylformamide (4ml) at 0 ℃ was slowly added sodium hydride (19mg, 0.801mmol) over 15 minutes. The suspension was warmed to room temperature. The mixture was stirred for 45 min and 4- (Boc-amino) butyl bromide (202mg, 0.801mmol) was added. The solution was stirred for 15 hours, then 0.25mL of methanol was added. Column chromatography was performed to provide the title compound.
Example 1286D
6- (4-Aminobutyl) -9-chloro-3, 3a, 4, 4 a-tetrahydro-2H-furo [2 ', 3': 2, 3] cyclobuta [1, 2-c ] quinolin-5 (6H) -one
The title compound was prepared as described in example 2D, replacing tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl [4- (9-chloro-5-oxo-2, 3, 3a, 4, 4a, 5-hexahydro-6H-furo [2 ', 3': 2, 3] cyclobuta (cyclobuta) [1, 2-c ] quinolin-6-yl) butyl ] carbamate.
Example 1286E
N- [4- (9-chloro-5-oxo-2, 3, 3a, 4, 4a, 5-hexahydro-6H-furo [2 ', 3': 2, 3] cyclobuta [1, 2-c ] quinolin-6-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 272B using 6- (4-aminobutyl) -9-chloro-3, 3a, 4, 4 a-tetrahydro-2H-furo [2 ', 3': 2, 3]Cyclobutanea [1, 2-c ]]Quinolin-5 (6H) -one instead of 4-amino-N-propylbenzamide, 1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine replaces the methyl isoindoline-5-carboxylate hydrochloride.1H NMR(400MHz，CDCl3)δppm 8.58(s，1H)，8.54(d，J＝4.9Hz，1H)，7.29(d，J＝4.9Hz，1H)，7.25(m，1H)，7.23(d，J＝2.6Hz，1H)，6.92(d，J＝8.9Hz，1H)，4.84(t，J＝5.6Hz，1H)，4.74(bs，4H)，4.46(t，J＝8.1Hz，1H)，4.22(m，1H)，4.05(m，1H)，3.91(m，1H)，3.39(m，3H)，2.93(m，1H)，2.31(m，1H)，2.22(m，1H)，1.84(m，1H)，1.69(m，5H)；MS(ESI(+))m/e 467(M+H)+。
Example 1287
N- {4- [ 7-chloro-1- (2-hydroxyethyl) -3-oxo-1, 3-dihydrocyclobuta (cyclobuta) [ c ] quinolin-4 (2H) -yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
To the N- [4- (9-chloro-5-oxo-2, 3, 3a, 4, 4a, 5-hexahydro-6H-furo [2 ', 3 ': 2, 3 ')]Cyclobutanea [1, 2-c ]]Quinolin-6-yl) butyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]To a solution of pyridine-2-carboxamide (30mg, 0.064mmol) in dimethylformamide (292. mu.l) and water (292. mu.l) was added sodium hydroxide (1.679. mu.l, 0.064 mmol). The solution was stirred for 18 hours, then 1M HCl was added dropwise to adjust the pH to 7. Column chromatography of the wet crude mixture provided the title compound. 1H NMR(400MHz，CDCl3)δppm 8.58(s，1H)，8.54(d，J＝5.1Hz，1H)，7.54(d，J＝2.4Hz，1H)，7.46(dd，J＝9.1，2.4Hz，1H)，7.37(d，J＝9.1Hz，1H)，7.25(m，1H)，5.06(t，J＝5.7Hz，1H)4.77(bs，2H)，4.75(bs，2H)，4.33(t，J＝7.4Hz，2H)，3.87(m，2H)，3.74(m，2H)，3.46(m，2H)，3.37(dd，J＝14.0，4.5Hz，1H)，2.86(dd，J＝14.0，1.3Hz，1H)，2.27(m，1H)，1.97(m，1H)，1.82(m，2H)，1.71(m，2H)；MS(ESI(+))m/e 467(M+H)+。
Example 1290
N- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting (R) - (tetrahydrofuran-2-yl) methylamine for 3-phenylprop-1-amine, and 6- (isoindoline-2-carboxamido) pyridazine-3-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ10.02(s，1H)，8.85(t，J＝6.1Hz，1H)，8.32(d，J＝9.3Hz，1H)，8.12(d，J＝9.3Hz，1H)，7.41-7.28(m，4H)，5.00-4.71(m，4H)，4.04(p，J＝6.2Hz，1H)，3.85-3.74(m，1H)，3.70-3.58(m，1H)，3.44-3.33(m，3H)，1.99-1.71(m，2H)，1.69-1.54(m，1H)；MS(ESI(+))m/e368(M+H)+。
Table 21.
The following examples were prepared essentially as in example 1C, substituting N- (4-aminophenyl) -1H-pyrrolo [3, 4-C ] pyridine-2 (3H) -carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 1369
N- { 7-oxo-7- [ (3-phenylpropyl) amino ] heptyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting 7- (isoindoline-2-carboxamido) heptanoic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 1373
N- (4- {2- [ (3-methylbutyryl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 1373A
N- (4- (2-aminoethyl) phenyl) isoindoline-2-carboxamide
The title compound was prepared as described in example 2D substituting tert-butyl (2- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } ethyl) carbamate for tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.
Example 1373B
N- (4- {2- [ (3-methylbutyryl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (2-aminoethyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and 3-methylbutyric acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6Temperature 90 ℃) δ 7.50-7.40(M, 2H), 7.40-7.24(M, 4H), 7.13-7.02(M, 2H), 4.76(s, 4H), 2.68(t, J ═ 7.3Hz, 2H), 2.07-1.84(M, 3H), 0.95-0.76(M, 6H), MS (ESI (+)) M/e 366(M + H)+。
Table 22.
The following examples were prepared essentially as described in example 1C, substituting N- (4- (2-aminoethyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 1404
N- (4- { [1- (2-cyclopropylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with 2-cyclopropylacetaldehyde instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide. 1HNMR (400MHz, pyridine-d)5. Temperature 90 ℃) δ ppm 8.54-8.58(m, 2H)8.08(s, 1H)7.72-7.77(m, 2H)7.10(d, J ═ 4.88Hz, 1H)7.01(d, J ═ 9.16Hz, 2H)4.82-4.88(m, 4H)3.71(s, 1H)2.74-2.82(m, 2H)2.43-2.50(m, 2H)2.22-2.31(m, 2H)1.97(s, 2H)1.79-1.90(m, 2H)1.35-1.47(m, 2H)0.70(s, 1H)0.36-0.45(m, 2H)0.05(q, J ═ 4.78Hz, 2H); MS (APCI (+)) M/e 407(M + H)+。
Example 1405
N- (4- { [1- (2-cyclopentylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with 2-cyclopentylacetaldehyde replacing isobutyraldehyde, N- (4-, (Piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide.1HNMR (400MHz, pyridine-d)5. Temperature 90 ℃) δ ppm 8.54-8.58(m, 2H)8.08(s, 1H)7.72-7.78(m, 2H)7.10(d, J ═ 4.88Hz, 1H)7.00-7.04(m, 2H)4.82-4.90(m, 4H)4.21-4.31(m, 1H)2.73-2.83(m, 2H)2.34-2.40(m, 2H)2.20-2.29(m, 2H)1.96-2.03(m, 2H)1.67-1.93(m, 5H)1.40-1.62(m, 6H)1.04-1.17(m, 2H); MS (APCI (+)) M/e 435(M + H) +。
Example 1406
N- (4- { [1- (2-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with 2-methylbutanal instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide.1HNMR (400MHz, pyridine-d)5. Temperature 90 ℃) δ ppm 8.52-8.58(m, 2H)8.08(s, 1H)7.74(d, J-8.85 Hz, 2H)7.10(d, J-4.58 Hz, 1H)6.97-7.05(m, 2H)4.84(d, J-6.71 Hz, 4H)2.72(d, J-10.68 Hz, 2H)2.13-2.26(m, 3H)2.01-2.07(m, 2H)1.91-2.00(m, 2H)1.83(s, 2H)1.54(s, 2H)1.14(s, 1H)0.81-0.95(m, 6H); MS (APCI (+)) M/e 409(M + H)+。
Example 1407
N- (4- { [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with tetrahydrofuran-3-carbaldehyde instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide. 1HNMR (400MHz, pyridine-d)5. Temperature 90 c.delta ppm 8.53-8.58(m, 1H)8.08(s,1H)7.70-7.77(m，2H)7.10(d，J＝5.19Hz，1H)7.01(d，J＝8.85Hz，2H)4.84(d，J＝7.63Hz，4H)4.19-4.27(m，1H)3.75-3.90(m，2H)3.67-3.72(m，1H)3.56(dd，J＝8.55，5.80Hz，1H)2.65-2.82(m，2H)2.31-2.45(m，1H)2.15-2.31(m，4H)1.71-2.00(m，5H)1.48-1.59(m，1H)；MS(APCI(+))m/e 423(M+H)+。
example 1408
N- (4- { [1- (3, 3-dimethylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with 3, 3-dimethylbutyraldehyde instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide.1HNMR (400MHz, pyridine-d)5. Temperature 90 ℃) δ ppm 8.52-8.58(m, 2H)8.09(s, 1H)7.71-7.78(m, 2H)7.10(d, J ═ 4.88Hz, 1H)6.99-7.04(m, 2H)4.84(dd, J ═ 8.39, 1.68Hz, 4H)3.85(d, J ═ 13.43Hz, 1H)2.75-2.85(m, 2H)2.38-2.47(m, 2H)2.21-2.34(m, 2H)1.98(d, J ═ 2.14Hz, 2H)1.78-1.91(m, 2H)1.39-1.49(m, 2H)0.84-0.92(m, 9H); MS (APCI (+)) M/e 423(M + H)+。
Example 1409
N- (4- { [1- (cyclohexylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with cyclohexanecarboxaldehyde instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c ]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide.1HNMR (400MHz, pyridine-d)5. Temperature 90 ℃) delta ppm 8.53-8.57(m, 2H)8.08(s, 1H)7.69-7.77(m, 2H)7.10(s, 1H)6.97-7.04(m, 2H)4.82-4.87(m, 4H)4.20-4.27(m, 1H)2.73(t, J ═ 10.68Hz, 2H)2.17-2.26(m, 2H)2.13(d, J ═ 7.02Hz, 2H)1.93-2.01(m, 2H)H)1.76-1.87(m，4H)1.55-1.72(m，3H)1.44-1.54(m，1H)1.09-1.29(m，3H)0.89(d，J＝12.51Hz，2H)；MS(APCI(+))m/e 435(M+H)+。
Example 1410
N- (4- { [1- (3-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with 3-methylbutanal instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide.1HNMR (400MHz, pyridine-d)5. Temperature 90 ℃) δ ppm 8.53-8.57(m, 2H)8.09(s, 1H)7.70-7.78(m, 2H)7.10(d, J ═ 5.19Hz, 1H)6.98-7.04(m, 2H)4.79-4.89(m, 4H)4.26(d, J ═ 3.66Hz, 1H)2.72-2.83(m, 2H)2.34-2.41(m, 2H)2.21-2.30(m, 2H)1.96-2.03(m, 2H)1.79-1.91(m, 2H)1.54-1.68(m, 1H)1.35-1.44(m, 2H)0.86-0.90(m, 6H); MS (APCI (+)) M/e 408(M + H) +。
Example 1411
N- (4- { [1- (cyclopentylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with cyclopentanecarboxaldehyde instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide.1HNMR (400MHz, pyridine-d)5. Temperature 90 ℃) δ ppm 8.53-8.57(m, 2H)8.08(s, 1H)7.70-7.77(m, 2H)7.10(d, J ═ 4.88Hz, 1H)6.97-7.05(m, 2H)4.84(dd, J ═ 8.54, 1.53Hz, 4H)4.23-4.27(m, 1H)2.75(d, J ═ 10.99Hz, 2H)2.18-2.29(m, 4H)2.04(s, 1H)1.94-2.02(m, 2H)1.77-1.90(m, 2H)1.65-1.76(m, 2H)1.42-1.59(m, 4H)1.17-1.32(m, 2H); MS (APCI (+)) M/e 420(M + H)+。
Example 1412
N- (4- { [1- (tetrahydrofuran-2-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with tetrahydrofuran-2-carbaldehyde instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide. 1HNMR (400MHz, pyridine-d)5. Temperature 90 ℃) δ ppm 8.53-8.59(m, 2H)8.07(s, 1H)7.73(d, J-9.16 Hz, 2H)7.10(d, J-5.49 Hz, 1H)6.97-7.02(m, 2H)4.80-4.87(m, 4H)4.03(d, J-11.60 Hz, 1H)3.77-3.84(m, 1H)3.61-3.69(m, 1H)2.88(d, J-41.81 Hz, 2H)2.25-2.63(m, 4H)1.97(s, 2H)1.77-1.91(m, 4H)1.64-1.76(m, 2H)1.44-1.58(m, 1H); MS (APCI (+)) M/e 423(M + H)+。
Example 1413
N- (4- { [1- (2-methylpropyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 429 with isobutyraldehyde instead of isobutyraldehyde, N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl) isoindoline-2-carboxamide.1H NMR (400MHz, pyridine-d)5. Temperature 90 ℃) δ ppm 8.49-8.60(m, 2H)8.09(s, 1H)7.68-7.80(m, 2H)7.10(d, J ═ 5.19Hz, 1H)6.96-7.04(m, 2H)4.85(s, 4H)4.21-4.28(m, 1H)2.65-2.79(m, 2H)2.13-2.24(m, 2H)2.06(m, 2H)1.98(s, 2H)1.77-1.88(m, 2H)1.67-1.77(m, 1H)0.89(d, J ═ 6.71Hz, 6H); MS (APCI (+)) M/e 395(M + H) +。
Example 1414
N- (4- { [1- (butanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide and 1-butanesulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.59(s, 1H)8.49(d, J ═ 4.88Hz, 1H)7.36-7.48(m, 3H)6.90(d, J ═ 8.85Hz, 2H)4.80(d, J ═ 6.10Hz, 4H)4.39-4.50(m, 1H)3.41-3.49(m, 2H)3.13-3.20(m, 2H)2.99-3.06(m, 2H)1.94-2.01(m, 2H)1.63-1.76(m, 4H)1.37-1.49(m, 2H)0.91(t, J ═ 7.48Hz, 3H); MS (APCI (+)) M/e 459(M + H)+。
Example 1415
N- (4- { [1- (cyclopropylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide and cyclopropylsulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride. 1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.57(s, 1H)8.48(d, J ═ 4.88Hz, 1H)7.40(d, J ═ 8.54Hz, 3H)6.90(d, J ═ 8.85Hz, 2H)4.79(d, J ═ 8.24Hz, 4H)4.39-4.49(m, 1H)3.44-3.51(m, 2H)3.17-3.23(m, 2H)2.54-2.58(m, 1H)1.95-2.03(m, 2H)1.68-1.78(m, 2H)0.91-1.07(m, 4H); MS (APCI (+)) M/e 442(M + H)+。
Example 1416
N- (4- { [1- (phenylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide and benzenesulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.59(s, 1H)8.49(d, J ═ 4.88Hz, 1H)7.77(d, J ═ 7.32Hz, 2H)7.71(t, J ═ 7.32Hz, 1H)7.65(t, J ═ 7.32Hz, 2H)7.44(d, J ═ 4.88Hz, 1H)7.35(d, J ═ 8.85Hz, 2H)6.79(d, J ═ 9.16Hz, 2H)4.79(d, J ═ 4.27Hz, 4H)4.29-4.37(m, 1H)3.22-3.25(m, 2H)2.92-3.06(m, 2H)1.87-2.04(m, 2H)1.61 (m, 1H) 1.79(m, 2H) 1.79; MS (APCI (+)) M/e 479(M + H)+。
Example 1417
N- [4- ({1- [ (4-fluorophenyl) sulfonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, (4-fluorophenyl) sulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.58(s, 1H)8.49(d, J ═ 4.88Hz, 1H)7.84(dd, J ═ 8.85, 5.19Hz, 2H)7.40-7.49(m, 3H)7.36(d, J ═ 8.85Hz, 2H)6.80(d, J ═ 8.85Hz, 2H)4.79(d, J ═ 4.88Hz, 4H)4.28-4.41(m, 1H)3.21-3.26(m, 2H)2.94-3.05(m, 2H)1.89-2.02(m, 2H)1.62-1.76(m, 2H); MS (APCI (+)) M/e 497(M + H)+。
Example 1418
N- (4- { [1- (ethanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, ethanesulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.58(s, 1H)8.48(d, J ═ 5.19Hz, 1H)7.40(d, J ═ 8.85Hz, 3H)6.90(d, J ═ 8.85Hz, 2H)4.79(d, J ═ 7.32Hz, 4H)4.39-4.48(m, 1H) 3.41-3.49.49 (m，2H)3.14-3.22(m，2H)3.05(q，J＝7.43Hz，2H)1.94-2.03(m，2H)1.64-1.78(m，2H)1.24(t，J＝7.32Hz，3H)；MS(APCI(+))m/e 431(M+H)+。
Example 1419
N- (4- { [1- (propan-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, isopropylsulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.59(s, 1H)8.49(d, J ═ 5.19Hz, 1H)7.36-7.47(m, 3H)6.89(d, J ═ 8.85Hz, 2H)4.80(d, J ═ 5.49Hz, 4H)4.40-4.49(m, 1H)3.46-3.55(m, 2H)3.33-3.36(m, 1H)3.15-3.24(m, 2H)1.93-2.01(m, 2H)1.62-1.74(m, 2H)1.25(d, J ═ 6.71Hz, 6H); MS (APCI (+)) M/e 445(M + H)+。
Example 1420
N- (4- { [1- (benzylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide, benzylsulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.58(s, 1H)8.48(d, J ═ 4.88Hz, 1H)7.31-7.46(m, 8H)6.87(d, J ═ 9.16Hz, 2H)4.79(d, J ═ 7.02Hz, 4H)4.38-4.44(m, 1H)4.36(s, 2H)3.34-3.38(m, 2H)3.07-3.16(m, 2H)1.82-1.90(m, 2H)1.57-1.71(m, 2H); MS (APCI (+)) M/e 493(M + H) +。
Example 1421
N- (4- { [1- (propylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide and 1-propanesulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.59(s, 1H)8.49(d, J ═ 4.88Hz, 1H)7.35-7.46(m, 3H)6.90(d, J ═ 8.85Hz, 2H)4.80(d, J ═ 5.80Hz, 4H)4.39-4.48(m, 1H)3.39-3.49(m, 2H)3.12-3.22(m, 2H)2.96-3.06(m, 2H)1.93-2.03(m, 2H)1.62-1.79(m, 4H)1.01(t, J ═ 7.48Hz, 3H); MS (APCI (+)) M/e 445(M + H)+。
Example 1422
N- (4- { [1- (thien-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 883 using N- (4- (piperidin-4-yloxy) phenyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of N- (4-aminophenyl) isoindoline-2-carboxamide and thiophene-2-sulfonyl chloride instead of (3-methoxyphenyl) methanesulfonyl chloride.1HNMR(400MHz，DMSO-D2O, temperature 90 ℃) δ ppm 8.58(s, 1H)8.49(d, J ═ 5.19Hz, 1H)7.96(d, J ═ 4.27Hz, 1H)7.63(d, J ═ 3.05Hz, 1H)7.44(d, J ═ 4.88Hz, 1H)7.37(d, J ═ 8.85Hz, 2H)7.23-7.30(m, 1H)6.81(d, J ═ 8.85Hz, 2H)4.79(d, J ═ 4.88Hz, 4H)4.29-4.43(m, 1H)3.31-3.38(m, 2H)2.97-3.09(m, 2H)1.93-2.06(m, 2H)1.65-1.81(m, 2H); MS (APCI (+)) M/e 485(M + H) +。
Example 1441
Trans-3- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] cyclobutanecarboxylic acid benzyl ester
Example 1441A
Trans-3- (tert-Butoxycarbonylamino) cyclobutanecarboxylic acid benzyl ester
A suspension of trans-3- (tert-butoxycarbonylamino) cyclobutanecarboxylic acid (0.5g, 2.323mmol) and potassium carbonate (0.321g, 2.323mmol) in dimethylformamide (2.323ml) was treated with (bromomethyl) benzene (0.401g, 2.346mmol) (added by syringe over 3 minutes). The reaction mixture was stirred at room temperature for 17 hours, and water was added. The suspension was filtered and the collected solid was washed with water and dried in vacuo to give the title compound.
Example 1441B
trans-3-Aminocyclobutanecarboxylic acid benzyl ester
The title compound was prepared as described in example 2D substituting benzyl trans-3- (tert-butoxycarbonylamino) cyclobutanecarboxylate for tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.
Example 1441C
Trans-3- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] cyclobutanecarboxylic acid benzyl ester
The title compound was prepared as described in example 272B substituting benzyl trans-3-aminocyclobutanecarboxylate for 4-amino-N-propylbenzamide, 1, 3-dihydro-2H-pyrrolo [3, 4-c) ]Pyridine replaces the methyl isoindoline-5-carboxylate hydrochloride.1H NMR(300MHz，DMSO-d6)δppm 8.56(s，1H)，8.47(d，J＝5.0Hz，1H)，7.43-7.31(m，6H)，6.68(d，J＝7.6Hz，1H)，5.14(s，2H)，4.65-4.58(m，4H)，4.41-4.29(m，1H)，3.11-2.99(m，1H)，2.46-2.25(m，4H)；MS(ESI(+))m/e352(M+H)+。
Example 1452
N- (4- {3- [ (3-methylbutyryl) amino ] oxetan-3-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1452A
2-methyl-N- (oxetan-3-ylidene) propane-2-sulfinamide
To a 250ml round bottom flask was added 2-methylpropane-2-sulfinamide (3.36g, 27.8mmol) and then titanium tetraethoxide (11.64ml, 55.5mmol) to a solution of oxetan-3-one (2g, 27.8mmol) in tetrahydrofuran (69.4ml) at room temperature. The mixture was stirred at 50 ℃ for 5 hours, cooled, and poured into brine. The suspension was filtered through a pad of celite eluting with ethyl acetate. The organics were combined, dried over sodium sulfate, filtered and concentrated in vacuo. The residue was purified by conventional phase flash column chromatography to give the title compound.
Example 1452B
N- (3- (4-bromophenyl) oxetan-3-yl) -2-methylpropane-2-sulfinamide
To a 50ml round bottom flask was added 1, 4-dibromobenzene (2.85g, 12.07mmol) in tetrahydrofuran (40.2 ml). The solution was cooled to-78 ℃ and n-butyllithium (4.51ml, 11.26mmol) was added dropwise. The mixture was stirred at-78 ℃ for 1 hour. A solution of 2-methyl-N- (oxetan-3-ylidene) propane-2-sulfinamide (1.41g, 8.05mmol) in tetrahydrofuran (ca. 1ml) was added, the reaction stirred for 10 minutes and allowed to warm to room temperature. Saturated ammonium chloride was added followed by water and dichloromethane. The aqueous layer was extracted twice with dichloromethane and the combined organics were dried over magnesium sulfate, filtered and concentrated in vacuo. The residue was purified by conventional phase flash column chromatography to give the title compound.
Example 1452C
N- (4- (3- (1, 1-Dimethylethylsulfonamido) oxetan-3-yl) phenyl) acetamide
To a 5ml microwave tube were added N- (3- (4-bromophenyl) oxetan-3-yl) -2-methylpropane-2-sulfinamide (436mg, 1.312mmol), cesium carbonate (1283mg, 3.94mmol) and acetamide (116mg, 1.968 mmol)/dioxane (6.5 ml). Xanthene (76mg, 0.131mmol) and tris (dibenzylideneacetone) dipalladium (0) (60.1mg, 0.066mmol) were added; the tube was purged with nitrogen and capped. The mixture was heated at 100 ℃ for 45 minutes. Aqueous workup, extraction with dichloromethane gave an organic layer which was dried over sodium sulfate, filtered and concentrated in vacuo. Conventional phase chromatography was performed to provide the title compound.
Example 1452D
N- (3- (4-aminophenyl) oxetan-3-yl) -2-methylpropane-2-sulfinamide
Claisen's base (potassium hydroxide, 12.7g in 9ml water and 33ml methanol) was added to N- (4- (3- (1, 1-dimethylethylsulfonamido) oxetan-3-yl) phenyl) acetamide (300mg, 0.966mmol) and the reaction was stirred at 90 ℃ for 2 h. The mixture was cooled to room temperature while adding water and ethyl acetate. The aqueous layer was extracted twice with ethyl acetate and the combined organics were dried over magnesium sulfate, filtered and concentrated in vacuo. The residue was purified by conventional phase flash column chromatography to give the title compound.
Example 1452E
N- (4- (3- (1, 1-Dimethylethylsulfonamido) oxetan-3-yl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 272B substituting N- (3- (4-aminophenyl) oxetan-3-yl) -2-methylpropane-2-sulfinamide for 4-amino-N-propylbenzamide and 1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine for methyl isoindoline-5-carboxylate hydrochloride.
Example 1452F
N- (4- (3-Aminooxetan-3-yl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
In a 20ml vial was added N- (4- (3- (1, 1-dimethylethylsulfonamido) oxetan-3-yl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide (253mg, 0.610mmol) and methanol (6.1 ml). 4N HCl/dioxane (229. mu.l, 0.916mmol) was added and the reaction was stirred for 2 hours. The mixture was concentrated in vacuo to give the title compound, which was used without further purification.
Example 1452G
N- (4- {3- [ (3-methylbutyryl) amino ] oxetan-3-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, using N- (4- (3-aminooxetan-3-yl) phenyl) -1H-pyrrolo [3, 4-C ] ]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and 3-methylbutyric acid instead of 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.84(s，1H)，8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.44(s，1H)，7.54(d，J＝8.7Hz，2H)，7.43(d，J＝4.8Hz，1H)，7.36(d，J＝8.8Hz，2H)，4.81(d，J＝6.5Hz，6H)，4.69(d，J＝6.5Hz，2H)，2.10-1.87(m，3H)，0.90(d，J＝6.4Hz，6H)；MS(ESI(+))m/e 395(M+H)+。
Example 1453
4- ({4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } sulfonyl) piperidine-1-carboxylic acid tert-butyl ester
Example 1453A
4- (4-Aminophenylthio) piperidine-1-carboxylic acid tert-butyl ester
To a 100ml round bottom flask were added 4-aminothiophenol (4.9g, 39.1mmol) and potassium carbonate (9.72g, 70.3mmol) in dimethylformamide (20 ml). Tert-butyl 4- (tosyloxy) piperidine-1-carboxylate (5g, 14.07mmol) was added and the reaction stirred in a sealed flask at 70 ℃ for 20 h. The mixture was cooled and filtered through a plug of silica gel using dichloromethane. The filtrate was concentrated in vacuo and chromatographed to give the title compound.
Example 1453B
4- (4-Acetylaminophenylthio) piperidine-1-carboxylic acid tert-butyl ester
To a 10ml round bottom flask was added 4- (4-aminophenylthio) piperidine-1-carboxylic acid tert-butyl ester (100mg, 0.324mmol) and triethylamine (249. mu.l, 1.783mmol) in dichloromethane (3242. mu.l). The mixture was cooled to-78 ℃ and acetyl chloride (1l 5. mu.l, 1.621mmol) was added. The solution was warmed to room temperature, stirred for 1 hour, and then diluted with water and additional dichloromethane. The aqueous phase was extracted twice with dichloromethane and the combined organics were dried over sodium sulfate, filtered and concentrated to give the title compound.
Example 1453C
4- (4-Acetylaminobenzenesulfonyl) piperidine-1-carboxylic acid tert-butyl ester
A10 mL round bottom flask was charged with tert-butyl 4- (4-acetamidophenylthio) piperidine-1-carboxylate (100mg, 0.285mmol) in dichloromethane (2.9 mL). The solution was cooled to-20 ℃ and mCPBA (192mg, 0.856mmol) was added. The reaction mixture was warmed to room temperature and treated with 1N aqueous NaOH. The aqueous layer was extracted with dichloromethane and the combined organics were dried over sodium sulfate, filtered and concentrated to give the title compound.
Example 1453D
4- (4-Aminobenzenesulfonyl) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 1452D, substituting 4- (4-acetamidophenylsulfonyl) piperidine-1-carboxylic acid tert-butyl ester for N- (4- (3- (1, 1-dimethylethylsulfonamido) oxetan-3-yl) phenyl) acetamide.
Example 1453E
4- ({4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } sulfonyl) piperidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 272B, substituting 4- (4-aminobenzenesulfonyl) piperidine-1-carboxylic acid tert-butyl ester for 4-ammonia1, 3-dihydro-2H-pyrrolo [3, 4-c ] methyl-N-propylbenzamide ]Pyridine is substituted for methyl isoindoline-5-carboxylate.1H NMR(300MHz，DMSO-d6)δ8.95(s，1H)，8.62(s，1H)，8.51(d，J＝5.0Hz，1H)，7.90-7.83(m，2H)，7.76-7.69(m，2H)，7.44(d，J＝5.1Hz，1H)，4.93-4.76(m，4H)，4.09-3.93(m，2H)，2.84-2.56(m，1H)，1.83(d，J＝10.8Hz，1H)，1.48-1.16(m，6H)；MS(ESI(+))m/e 431(M+H)+。
Example 1454
N- {4- [4- (propylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1454A
1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) piperidine-4-carboxylic acid
The title compound was prepared as described in example 1246, substituting piperidine-4-carboxylic acid methyl ester for azetidine-3-carboxylic acid methyl ester hydrochloride in example 1246A.
Example 1454B
N- {4- [4- (propylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting propan-1-amine for 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-formylamino) phenyl) piperidine-4-carboxylic acid is substituted for 4- (isoindoline-2-formylamino) benzoic acid.1H NMR(300MHz，DMSO-d6)δppm 8.60(s，1H)，8.49(d，J＝5.0Hz，1H)，8.19(s，1H)，7.77(t，J＝5.6Hz，1H)，7.42(d，J＝5.1Hz，1H)，7.39-7.33(m，2H)，6.89-6.83(m，2H)，4.77(d，J＝6.2Hz，4H)，3.64-3.56(m，2H)，3.05-2.94(m，2H)，2.63-2.52(m，2H)，2.28-2.14(m，1H)，1.79-1.59(m，4H)，1.47-1.33(m，2H)，0.84(t，J＝7.4Hz，3H)；MS(ESI(+))m/e408(M+H)+。
Table 23.
The following examples are prepared essentially as described in example 1C, substituting the appropriate amine for 3-phenylpropan-1-amine, 1- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-C ] pyridine-2-carboxamido) phenyl) piperidine-4-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.
Example 1472
N- (4- { (4R) -4- [ (2-Methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Reacting N- (4- {4- [ (2-methylpropanoyl) amino]Cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]The racemic mixture of pyridine-2-carboxamide (250mg) was dissolved in methanol and separated using SCF-LC (ChiralPak AD-H21X 250mm column) to provide N- (4- { (4R) -4- [ (2-methylpropanoyl) amino]Cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(300MHz，DMSO-d6)δ8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.41(s，1H)，7.66(d，J＝7.6Hz，1H)，7.56-7.48(m，2H)，7.43(d，J＝5.1Hz，1H)，7.37-7.29(m，2H)，6.02(bs，1H)，4.84-4.77(m，4H)，3.89-3.73(m，1H)，2.44(ddd，J＝12.7，8.7，4.6Hz，2H)，2.41-2.26(m，2H)，2.14-1.97(m，1H)，1.93-1.81(m，1H)，1.67-1.49(m，1H)，1.00(dd，J＝6.8，2.4Hz，6H)；MS(ESI(+))m/e405(M+H)+。
Example 1473
N- (4- { (4S) -4- [ (2-Methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Reacting N- (4- {4- [ (2-methylpropanoyl) amino]Cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]The racemic mixture of pyridine-2-carboxamide (250mg) was dissolved in methanol and separated using SCF-LC (ChiralPak AD-H21X 250mm column) to provide N- (4- { (4S) -4- [ (2-methylpropanoyl) amino]Cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(300MHz，DMSO-d6)δ8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.41(s，1H)，7.66(d，J＝7.6Hz，1H)，7.56-7.49(m，2H)，7.43(d，J＝5.1Hz，1H)，7.37-7.29(m，2H)，6.05-5.99(m，1H)，4.84-4.77(m，4H)，3.89-3.73(m，1H)，2.47-2.39(m，1H)，2.41-2.30(m，2H)，2.11-1.97(m，1H)，1.93-1.82(m，1H)，1.67-1.50(m，1H)，1.00(dd，J＝6.8，2.4Hz，6H)；MS(ESI(+))m/e405(M+H)+。
Example 1474
N- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 1474A
3- (2-hydroxyethyl) azetidine-1-carboxylic acid tert-butyl ester
A solution of 2- (1- (tert-butoxycarbonyl) azetidin-3-yl) acetic acid (1g, 4.65mmol) in tetrahydrofuran (5ml) was cooled to 0 ℃ and treated dropwise (using a syringe) with borane tetrahydrofuran complex (7.00ml, 7 mmol). After 1 hour at 0 ℃, the solution was warmed to room temperature, stirred overnight, and then quenched with 20ml of 1M aqueous NaOH. The separated aqueous layer was extracted with ether (2 × 15ml), dried over magnesium sulfate, filtered, and concentrated to give the title compound, which was used without purification.
Example 1474B
3- (2-oxoethyl) azetidine-1-carboxylic acid tert-butyl ester
Dimethyl sulfoxide (792. mu.l, 11.16mmol) was added dropwise to a solution of oxalyl chloride (488. mu.l, 5.58mmol) in dichloromethane (40 ml) at-78 ℃ using a syringe. The mixture was stirred at-78 ℃ for 15 minutes while adding dropwise a solution of 3- (2-hydroxyethyl) azetidine-1-carboxylic acid tert-butyl ester (936mg, 4.65mmol) in 10ml dichloromethane via syringe. After 1 h at-78 deg.C, triethylamine (3241. mu.l, 23.25mmol) was added and the suspension was warmed to room temperature and stirred for an additional 1 h. The mixture was quenched with water (25ml) and saturated aqueous potassium carbonate (10ml), stirred vigorously, and separated. The aqueous layer was extracted with dichloromethane (2 × 20ml) and the combined organic layers were dried over magnesium sulfate, filtered and concentrated. Flash chromatography of the crude product afforded the title compound.
Example 1474C
3- (3-cyanoallyl) azetidine-1-carboxylic acid tert-butyl ester
To a solution of 1M potassium tert-butoxide in tetrahydrofuran (3694. mu.l, 3.69mmol) at 0 ℃ was added dropwise, using a syringe, a solution of diethyl cyanomethylphosphonate (570. mu.l, 3.52mmol) in 5ml of tetrahydrofuran. The reaction mixture was warmed to room temperature and then cooled again to 0 ℃. Using a syringe, this solution was treated dropwise with tert-butyl 3- (2-oxoethyl) azetidine-1-carboxylate (701mg, 3.52mmol) in 2ml tetrahydrofuran, then warmed to room temperature. After stirring overnight, the gelatinous mixture was quenched with water (20ml) and extracted with ethyl acetate (2 × 20 ml); the organic layer was washed with brine (20ml), dried over magnesium sulfate, filtered and concentrated. Flash chromatography of the liquid residue gave a 1: 1 mixture of the E/Z isomers of the title compound.
Example 1474D
3- (4-Aminobutyl) azetidine-1-carboxylic acid tert-butyl ester
In a 20mL pressure bottle, add 7M NH3-CH3OH (10ml) was added to a slurry of 3- (3-cyanoallyl) azetidine-1-carboxylic acid tert-butyl ester (640mg, 2.88mmol) and Ra-Ni 2800 water (881mg, 6.75 mmol). The mixture was stirred under 30psi of hydrogen at room temperature for 16 hours. The mixture was filtered through a polypropylene membrane, concentrated by rotary evaporation, and dried in vacuo to provide the title compound, which was used without purification.
Example 1474E
3- (4- (isoindoline-2-carboxamido) butyl) azetidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 344A, substituting tert-butyl 3- (4-aminobutyl) azetidine-1-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate.
Example 1474F
N- (4- (azetidin-3-yl) butyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D, substituting 3- (4- (isoindoline-2-carboxamido) butyl) azetidine-1-carboxylic acid tert-butyl ester for 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate.
Example 1474G
N- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 278, substituting benzoyl chloride for acetyl chloride and N- (4- (azetidin-3-yl) butyl) isoindoline-2-carboxamide for 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindolineIndole-2-carboxamide.1H NMR(300MHz，DMSO-d6)δ7.67-7.57(m，2H)，7.57-7.39(m，3H)，7.39-7.23(m，4H)，6.28(s，1H)，4.56(s，4H)，4.34(t，J＝8.3Hz，1H)，4.11(t，J＝9.0Hz，1H)，4.01-3.82(m，1H)，3.65(dd，J＝9.8，5.8Hz，1H)，3.07(dd，J＝12.7，6.8Hz，2H)，2.66-2.53(m，1H)，1.59(dd，J＝15.3，7.7Hz，2H)，1.51-1.36(m，2H)，1.25(dd，J＝13.5，6.4Hz，2H)；MS(ESI(+))m/e 378(M+H)+。
Example 1475
N- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1475A
3- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) butyl) azetidine-1-carboxylic acid tert-butyl ester
The title compound was prepared as described in example 344A, substituting tert-butyl 3- (4-aminobutyl) azetidine-1-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate and 1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine for isoindoline.
Example 1475B
N- (4- (azetidin-3-yl) butyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 2D, substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 3- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) butyl) azetidine-1-carboxylate.
Example 1475C
N- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
As in example 278The title compound is prepared by substituting benzoyl chloride for acetyl chloride, N- (4- (azetidin-3-yl) butyl) -1H-pyrrolo [3, 4-c]Pyridine-2 (3H) -carboxamide instead of 5-amino-N- (4- (propylcarbamoyl) phenyl) isoindoline-2-carboxamide.1HNMR(300MHz，DMSO-d6)δ8.55(s，1H)，8.46(d，J＝5.0Hz，1H)，7.67-7.55(m，2H)，7.55-7.34(m，4H)，6.37(t，J＝5.5Hz，1H)，4.60(d，J＝2.3Hz，4H)，4.35(t，J＝8.3Hz，1H)，4.11(t，J＝9.1Hz，1H)，3.96-3.83(m，1H)，3.65(dd，J＝9.7，5.7Hz，1H)，3.07(dd，J＝12.8，6.7Hz，2H)，2.65-2.53(m，1H)，1.59(dd，J＝15.2，7.6Hz，2H)，1.43(dd，J＝14.4，7.2Hz，2H)，1.34-1.09(m，2H)；MS(ESI(+))m/e 379(M+H)+。
Example 1476
N- [ trans-3- (benzylcarbamoyl) cyclobutyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1476A
Trans-3- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) cyclobutanecarboxylic acid
The title compound was prepared as described in example 272A substituting benzyl trans-3- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] cyclobutanecarboxylate for 4-nitro-N-propylbenzamide.
Example 1476B
N- [ trans-3- (benzylcarbamoyl) cyclobutyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C substituting benzylamine for 3-phenylpropan-1-amine, trans-3- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-carboxamido) cyclobutanecarboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid. 1H NMR(400MHz，DMSO-d6)δppm 8.56(s，1H)，8.47(d，J＝5.0Hz，1H)，8.26(t，J＝5.9Hz，1H)，7.39(d，J＝5.1Hz，1H)，7.36-7.28(m，2H)，7.27-7.20(m，3H)，6.60(d，J＝7.6Hz，1H)，4.65-4.59(m，4H)，4.45-4.29(m，1H)，4.28(d，J＝5.9Hz，2H)，2.96-2.84(m，1H)，2.41-2.29(m，2H)，2.30-2.15(m，2H)；MS(ESI(+))m/e 351(M+H)+。
Example 1477
N- { trans-3- [ (2-phenylethyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C substituting 2-phenylethylamine for 3-phenylpropan-1-amine, trans-3- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-carboxamido) cyclobutanecarboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm 8.56(s，1H)，8.47(d，J＝5.0Hz，1H)，7.80(t，J＝5.6Hz，1H)，7.39(d，J＝5.1Hz，1H)，7.33-7.24(m，2H)，7.23-7.16(m，3H)，6.57(d，J＝7.6Hz，1H)，4.65-4.58(m，4H)，4.38-4.24(m，1H)，3.33-3.23(m，2H)，2.84-2.74(m，1H)，2.72(t，J＝7.3Hz，2H)，2.32-2.22(m，2H)，2.24-2.09(m，2H)；MS(ESI(+))m/e 365(M+H)+。
Example 1478
N- { trans-3- [ (3-phenylpropyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C substituting 3-phenylpropylamine for 3-phenylpropan-1-amine, trans-3- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-carboxamido) cyclobutanecarboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(400MHz，DMSO-d6)δppm 8.56(s，1H)，8.47(d，J＝5.0Hz，1H)，7.75(t，J＝5.5Hz，1H)，7.38(d，J＝5.1Hz，1H)，7.32-7.24(m，2H)，7.24-7.13(m，3H)，6.58(d，J＝7.6Hz，1H)，4.66-4.55(m，4H)，4.41-4.27(m，1H)，3.11-3.03(m，2H)，2.89-2.75(m，1H)，2.62-2.52(m，2H)，2.39-2.25(m，2H)，2.26-2.11(m，2H)，1.76-1.63(m，2H)；MS(ESI(+))m/e379(M+H)+。
Example 1525
N- [4- (cis-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1525A
4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) cyclohexylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 979A substituting tert-butyl 4- (4- (isoindoline-2-carboxamido) phenyl) -5, 6-dihydropyridine-1 (2H) -carboxylate with tert-butyl 4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) cyclohex-3-enylcarbamate.
Example 1525B
N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide
The title compound was prepared as described in example 2D substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (4- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) phenyl) cyclohexylcarbamate.
Example 1525C
N- [4- (cis-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide replaces 3-phenylpropan-1-amine, and 2- (2-methoxyethoxy) acetic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- [4- (cis-4- { [ (2-methoxyethoxy) N) Acetyl group]Amino } cyclohexyl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(501MHz，DMSO-d6)δ8.59(bs，1H)，8.51-8.45(m，1H)，8.32(bs，1H)，7.44(dd，J＝11.5，5.2Hz，3H)，7.40(t，J＝7.6Hz，1H)，7.17-7.11(m，2H)，4.81-4.74(m，4H)，4.03-3.96(m，1H)，3.90(d，J＝2.2Hz，2H)，3.63-3.58(m，2H)，3.52-3.46(m，2H)，3.27-3.23(m，3H)，1.80-1.30(m，8H)；MS(ESI(+))m/e 453(M+H)+。
Example 1526
N- [4- (trans-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide replaces 3-phenylpropan-1-amine, and 2- (2-methoxyethoxy) acetic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- [4- (trans-4- { [ (2-methoxyethoxy) acetyl ] acetyl]Amino } cyclohexyl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(501MHz，DMSO-d6)δ8.58(s，1H)，8.48(d，J＝5.0Hz，1H)，8.31(s，1H)，7.50-7.39(m，4H)，7.15-7.09(m，2H)，4.81-4.74(m，4H)，3.85(s，2H)，3.74-3.58(m，1H)，3.58-3.55(m，2H)，3.49-3.46(m，2H)，3.28(s，3H)，2.45-2.37(m，1H)，1.89-1.82(m，2H)，1.83-1.75(m，2H)，1.58-1.42(m，2H)，1.44-1.29(m，2H)；MS(ESI(+))m/e 453(M+H)+。
Example 1527
N- [4- (cis-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3 ]，4-c]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and (S) -tetrahydrofuran-2-carboxylic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- [4- (cis-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl]Amino } cyclohexyl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(501MHz，DMSO-d6)δ8.59(s，1H)，8.48(d，J＝5.0Hz，1H)，8.32(s，1H)，7.47-7.38(m，4H)，7.17-7.12(m，2H)，4.81-4.75(m，4H)，4.29-4.22(m，1H)，3.94-3.86(m，2H)，3.77(t，J＝7.1Hz，1H)，2.14-2.02(m，1H)，1.88-1.78(m，3H)，1.70(dd，J＝22.1，8.6Hz，3H)，1.63(t，J＝17.3Hz，6H)；MS(ESI(+))m/e 435(M+H)+。
Example 1528
N- [4- (trans-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and (S) -tetrahydrofuran-2-carboxylic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- [4- (trans-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl]Amino } cyclohexyl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(501MHz，DMSO-d6)δ8.58(bs，1H)，8.51-8.45(m，1H)，8.30(bs，1H)，7.53-7.45(m，1H)，7.42(d，J＝8.3Hz，2H)，7.14-7.08(m，2H)，4.81-4.74(m，4H)，4.20-4.13(m，1H)，3.92-3.85(m，1H)，3.78-3.71(m，1H)，3.66-3.58(m，1H)，2.39(s，1H)，2.09(dd，J＝10.8，6.4Hz，1H)，1.79(s，7H)，1.62(s，1H)，1.45(dd，J＝26.5，15.7Hz，4H)；MS(ESI(+))m/e 435(M+H)+。
Example 1529
N- [4- (cis-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and (R) -tetrahydrofuran-2-carboxylic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- [4- (cis-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ]Amino } cyclohexyl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(501MHz，DMSO-d6)δ8.55(t，J＝21.5Hz，1H)，8.46(s，1H)，8.32(d，J＝9.4Hz，1H)，7.47-7.37(m，4H)，7.14(bs，2H)，4.77(bs，4H)，4.29-4.20(m，1H)，3.96-3.84(m，2H)，3.80-3.71(m，1H)，2.12-2.01(m，1H)，1.76(d，J＝48.5Hz，4H)，1.60(s，7H)；MS(ESI(+))m/e 435(M+H)+。
Example 1530
N- [4- (trans-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and (R) -tetrahydrofuran-2-carboxylic acid instead of 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- [4- (trans-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl]Amino } cyclohexyl) phenyl]-1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1H NMR(501MHz，DMSO-d6)δ8.58(bs，1H)，8.50-8.45(m，1H)，8.31(bs，1H)，7.52-7.46(m，1H)，7.45-7.39(m，3H)，7.14-7.08(m，2H)，4.81-4.74(m，4H)，4.20-4.13(m，1H)，3.92-3.84(m，1H)，3.78-3.70(m，1H)，3.66-3.57(m，1H)，2.43-2.34(m，1H)，2.14-2.02(m，1H)，2.04-1.52(m，7H)，1.54-1.24(m，4H)；MS(ESI(+))m/e 435(M+H)+。
Example 1531
N- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
Example 1531A
6- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) pyridazine-3-carboxylic acid methyl ester
Methyl 6-aminopyridazine-3-carboxylate (2g, 13.06mmol) was suspended in dichloromethane (50ml) and then anhydrous pyridine (1.265ml, 15.67mmol) was added under nitrogen. To this suspension was added by syringe a solution of 4-nitrophenyl chloroformate (2.99g, 14.37mmol) in dichloromethane at ambient temperature. The mixture was stirred overnight to give a suspension which was concentrated to half volume under a stream of nitrogen. 2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine dihydrochloride (2.52g, 13.06mmol) was dissolved in 30ml of dimethylformamide (containing triisopropylethylamine (6.84ml, 39.2mmol)) and added to the carbamate mixture by syringe. After stirring the mixture overnight, most of the solvent was removed in vacuo and water was added; and the resulting suspension was stirred for 30 minutes, filtered to give a solid, which was washed with water. Flash chromatography of the dried solid afforded the title compound.
Example 1531B
6- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) pyridazine-3-carboxylic acid
The title compound was prepared as described in example 1B substituting methyl 6- (2, 3-dihydro-1H-pyrrolo [3, 4-c ] pyridine-2-carboxamido) pyridazine-3-carboxylate for methyl 4- (isoindoline-2-carboxamido) benzoate.
Example 1531C
N- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting (2S) -tetrahydrofuran-2-ylmethylamine for 3-phenylpropan-1-amine, 6- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-formylamino) pyridazine-3-carboxylic acid is substituted for 4- (isoindoline-2-formylamino) benzoic acid.1H NMR(300MHz，DMSO-d6)δ10.09(s，1H)，8.81(t，J＝6.1Hz，1H)，8.62(s，1H)，8.51(d，J＝5.0Hz，1H)，8.31(d，J＝9.3Hz，1H)，8.12(d，J＝9.3Hz，1H)，7.44(d，J＝5.1Hz，1H)，5.05-4.76(m，4H)，4.04(p，J＝6.2Hz，1H)，3.85-3.74(m，1H)，3.70-3.59(m，1H)，3.45-3.31(m，2H)，1.99-1.72(m，3H)，1.69-1.54(m，1H)；MS(ESI(+))m/e 369(M+H)+。
Example 1542
N- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting (2R) -tetrahydrofuran-2-ylmethylamine for 3-phenylpropan-1-amine, 6- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-formylamino) pyridazine-3-carboxylic acid is substituted for 4- (isoindoline-2-formylamino) benzoic acid.1H NMR(300MHz，DMSO-d6)δ10.09(bs，1H)，8.81(t，J＝6.1Hz，1H)，8.61(s，1H)，8.51(d，J＝5.0Hz，1H)，8.31(d，J＝9.3Hz，1H)，8.12(d，J＝9.3Hz，1H)，7.44(d，J＝5.1Hz，1H)，5.05-4.76(m，4H)，4.04(p，J＝6.2Hz，1H)，3.85-3.74(m，1H)，3.70-3.59(m，1H)，3.35(d，J＝25.7Hz，2H)，1.99-1.72(m，3H)，1.69-1.54(m，1H)；MS(ESI(+))m/e369(M+H)+。
Example 1543
N- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting tetrahydro-2H-pyran-4-ylmethylamine for 3-phenylpropan-1-amine, 6- (2, 3-bis-methylaminehydro-1H-pyrrolo [3, 4-c]Pyridine-2-formylamino) pyridazine-3-carboxylic acid is substituted for 4- (isoindoline-2-formylamino) benzoic acid.1H NMR(300MHz，DMSO-d6)δ10.06(s，1H)，9.00(t，J＝6.2Hz，1H)，8.62(s，1H)，8.51(d，J＝5.0Hz，1H)，8.29(d，J＝9.3Hz，1H)，8.11(d，J＝9.3Hz，1H)，7.44(d，J＝5.1Hz，1H)，4.96-4.89(m，4H)，3.89-3.79(m，2H)，3.22(d，J＝2.6Hz，3H)，1.96-1.75(m，1H)，1.64-1.53(m，2H)，1.31-1.10(m，2H)；MS(ESI(+))m/e 383(M+H)+。
Example 1544
N- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c1 pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting cyclopentylmethylamine for 3-phenylpropan-1-amine, 6- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-formylamino) pyridazine-3-carboxylic acid is substituted for 4- (isoindoline-2-formylamino) benzoic acid.1H NMR(300MHz，DMSO-d6)δ10.03(bs，1H)，8.95(t，J＝6.1Hz，1H)，8.62(s，1H)，8.51(d，J＝5.0Hz，1H)，8.29(d，J＝9.3Hz，1H)，8.11(d，J＝9.3Hz，1H)，7.44(d，J＝5.1Hz，1H)，4.99-4.75(m，4H)，3.28-3.20(m，2H)，2.31-2.13(m，1H)，1.75-1.38(m，6H)，1.39-1.18(m，2H)；MS(ESI(+))m/e367(M+H)+。
Example 1545
N- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, substituting tetrahydrofuran-3-ylmethylamine for 3-phenylpropan-1-amine, 6- (2, 3-dihydro-1H-pyrrolo [3, 4-C)]Pyridine-2-formylamino) pyridazine-3-carboxylic acid is substituted for 4- (isoindoline-2-formylamino) benzoic acid. 1H NMR(300MHz，DMSO-d6)δ10.05(s，1H)，9.13(t，J＝6.1Hz，1H)，8.62(s，1H)，8.51(d，J＝5.0Hz，1H)，8.30(d，J＝9.3Hz，1H)，8.12(d，J＝9.3Hz，1H)，7.44(d，J＝5.1Hz，1H)，5.05-4.76(m，4H)，3.80-3.57(m，4H)，3.48(dd，J＝12.1，6.8Hz，1H)，3.37-3.31(m，1H)，2.62-2.52(m，1H)，2.01-1.80(m，1H)，1.71-1.56(m，1H)；MS(ESI(+))m/e 369(M+H)+。
EXAMPLE 1546
N- {6- [ (bicyclo [2.2.1] hept-2-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
The title compound was prepared as described in example 1C, using bicyclo [2.2.1]Hept-2-ylmethylamine as a substitute for 3-phenylpropan-1-amine, 6- (2, 3-dihydro-1H-pyrrolo [3, 4-c)]Pyridine-2-formylamino) pyridazine-3-carboxylic acid is substituted for 4- (isoindoline-2-formylamino) benzoic acid.1H NMR(300MHz，DMSO-d6)δ10.05(bs，1H)，8.92(d，J＝42.7Hz，1H)，8.61(s，1H)，8.51(d，J＝5.0Hz，1H)，8.29(d，J＝9.3Hz，1H)，8.10(d，J＝9.3Hz，1H)，7.47-7.41(m，1H)，5.07-4.74(m，4H)，3.23-2.84(m，2H)，2.30-2.02(m，3H)，1.86-1.57(m，2H)，1.58-0.99(m，6H)；MS(ESI(+))m/e 393(M+H)+。
Example 1547
N- (4- { trans-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and isobutyric acid instead of 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- (4- { trans-4- [ (2-methylpropanoyl) amino]Cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1HNMR(300MHz，DMSO-d6)δ8.60(s，1H)，8.50(d，J＝5.0Hz，1H)，8.32(s，1H)，7.58(d，J＝7.8Hz，1H)，7.48-7.40(m，3H)，7.17-7.09(m，2H)，4.82-4.76(m，4H)，3.65-3.47(m，1H)，2.41-2.23(m，2H)，1.93-1.69(m，4H)，1.62-1.38(m，2H)，1.39-1.12(m，2H)，0.99(d，J＝6.8Hz，6H)；MS(ESI(+))m/e 407(M+H)+。
Example 1548
N- (4- { cis-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide instead of 3-phenylpropan-1-amine and isobutyric acid instead of 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- (4- { cis-4- [ (2-methylpropanoyl) amino]Cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1HNMR(300MHz，DMSO-d6)δ8.60(s，1H)，8.50(d，J＝5.0Hz，1H)，8.33(s，1H)，7.68-7.61(m，1H)，7.49-7.40(m，3H)，7.21-7.14(m，2H)，4.83-4.76(m，4H)，3.98-3.90(m，1H)，1.97-1.49(m，9H)，1.04-0.97(m，6H)；MS(ESI(+))m/e 407(M+H)+。
Example 1549
N- (4- { cis-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide replaces 3-phenylpropan-1-amine, and cyclohexanecarboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- (4- { cis-4- [ (cyclohexylcarbonyl) amino]Cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1HNMR(300MHz，DMSO-d6)δ8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.33(s，1H)，7.66-7.59(m，1H)，7.47(s，1H)，7.47-7.40(m，2H)，7.21-7.14(m，2H)，4.83-4.76(m，4H)，3.98-3.90(m，1H)，2.45(s，1H)，2.31-2.19(m，1H)，1.89-1.46(m，12H)，1.46-1.05(m，6H)；MS(ESI(+))m/e447(M+H)+。
Example 1550
N- (4- { trans-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide replaces 3-phenylpropan-1-amine, and cyclohexanecarboxylic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- (4- { trans-4- [ (cyclohexylcarbonyl) amino]Cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1HNMR(300MHz，DMSO-d6)δ8.60(s，1H)，8.49(d，J＝5.0Hz，1H)，8.32(s，1H)，7.54(d，J＝7.9Hz，1H)，7.47-7.40(m，3H)，7.16-7.09(m，2H)，4.82-4.75(m，4H)，3.62-3.42(m，1H)，2.42-2.33(m，1H)，2.12-1.99(m，1H)，1.87-1.61(m，8H)，1.55-1.37(m，3H)，1.38-1.08(m，7H)；MS(ESI(+))m/e 447(M+H)+。
Example 1551
N- (4- { trans-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide replaces 3-phenylpropan-1-amine, and 2-cyclopropylacetic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- (4- { trans-4- [ (cyclopropylacetyl) amino group]Cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1HNMR(300MHz，DMSO-d6)δ8.60(s，1H)，8.50(d，J＝5.0Hz，1H)，8.32(s，1H)，7.59(d，J＝7.8Hz，1H)，7.48-7.40(m，3H)，7.11(s，2H)，4.82-4.76(m，4H)，3.66-3.50(m，1H)，2.40(t，J＝10.1Hz，1H)，1.94(t，J＝11.8Hz，1H)，1.83(dd，J＝23.4，12.2Hz，4H)，1.61-1.39(m，2H)，1.40-1.18(m，3H)，1.04-0.83(m，1H)，0.46-0.33(m，2H)，0.18-0.07(m，2H)；MS(ESI(+))m/e 419(M+H)+。
Example 1552
N- (4- { cis-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide
A1: 1 cis/trans mixture of the title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohexyl) phenyl) -1H-pyrrolo [3, 4-C ] as]Pyridine-2 (3H) -carboxamide replaces 3-phenylpropan-1-amine, and 2-cyclopropylacetic acid replaces 4- (isoindoline-2-carboxamido) benzoic acid. HPLC separation of the cis/trans isomer provides N- (4- { cis-4- [ (cyclopropylacetyl) amino group]Cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c]Pyridine-2-carboxamide.1HNMR(300MHz，DMSO-d6)δ8.61(s，1H)，8.50(d，J＝5.0Hz，1H)，8.33(s，1H)，7.67-7.60(m，1H)，7.49-7.40(m，3H)，7.21-7.13(m，2H)，4.83-4.76(m，4H)，4.02-3.92(m，1H)，2.06(d，J＝7.0Hz，2H)，1.84-1.65(m，4H)，1.65-1.47(m，4H)，1.25-0.90(m，1H)，0.47-0.34(m，2H)，0.23-0.11(m，2H)；MS(ESI(+))m/e 419(M+H)+。
Example 1553
N- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
Example 1553A
4- (4-Nitrophenyl) cyclohex-3-enylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 1018B with 4, 4, 5, 5-tetramethyl-2- (4-nitrophenyl) -1, 3, 2-dioxaborolan substituting N- (4- (4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl) phenyl) -1H-pyrrolo [3, 4-c ] pyridine-2 (3H) -carboxamide.
Example 1553B
4- (4-aminophenyl) cyclohex-3-enylcarbamic acid tert-butyl ester
Tert-butyl 4- (4-nitrophenyl) cyclohex-3-enylcarbamate (2.55g, 8.01mmol) was suspended in ethanol (30ml), followed by the addition of sodium sulfide nonahydrate (10.37ml, 80mmol) (dissolved in water (30 ml)). Heating the mixture to 80 deg.C for 1.5 hr, and extracting with dichloromethane; the combined organic layers were dried over magnesium sulfate, filtered, and concentrated to give the title compound.
Example 1553C
4- (4- (isoindoline-2-carboxamido) phenyl) cyclohex-3-enylcarbamic acid tert-butyl ester
The title compound was prepared as described in example 272B substituting tert-butyl 4- (4-aminophenyl) cyclohex-3-enylcarbamate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.
Example 1553D
N- (4- (4-aminocyclohex-1-enyl) phenyl) isoindoline-2-carboxylic acid amide
The title compound was prepared as described in example 2D substituting tert-butyl 4- ((4- (5-fluoroisoindoline-2-carboxamido) benzamido) methyl) benzylcarbamate with tert-butyl 4- (4- (isoindoline-2-carboxamido) phenyl) cyclohex-3-enylcarbamate.
Example 1553E
N- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, using N- (4- (4-aminocyclohex-1-enyl) benzeneYl) isoindoline-2-carboxamide instead of 3-phenylpropan-1-amine and isobutyric acid instead of 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.36(s，1H)，7.70(d，J＝7.6Hz，1H)，7.54(d，J＝2.1Hz，2H)，7.46-7.23(m，6H)，6.06-5.96(m，1H)，4.76(s，4H)，3.85-3.75(m，1H)，2.43-2.26(m，3H)，2.11-1.96(m，1H)，1.95-1.75(m，1H)，1.69-1.48(m，1H)，1.10-0.82(m，6H)；MS(ESI(+))m/e 404(M+H)+。
Example 1554
N- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (4-aminocyclohex-1-enyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and (2R) -tetrahydrofuran-2-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.36(s，1H)，7.61(dt，J＝9.2，4.6Hz，1H)，7.58-7.45(m，2H)，7.49-7.23(m，6H)，6.02(bs，1H)，4.77(s，4H)，4.25-4.16(m，1H)，3.97-3.66(m，3H)，2.42-2.24(m，1H)，2.26-1.98(m，3H)，1.98-1.53(m，6H)；MS(ESI(+))m/e 432(M+H)+。
Example 1555
N- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (4-aminocyclohex-1-enyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and (2S) -tetrahydrofuran-2-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.37(s，1H)，7.63(dd，J＝8.2，3.5Hz，1H)，7.57-7.50(m，2H)，7.49-7.23(m，6H)，6.04-5.96(m，1H)，4.76(s，4H)，4.25-4.16(m，1H)，3.96-3.67(m，4H)，2.38-2.29(m，1H)，2.27-1.99(m，3H)，1.97-1.56(m，5H)；MS(ESI(+))m/e 432(M+H)+。
Example 1556
N- (4- {4- [ (cyclopentylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (4-aminocyclohex-1-enyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and cyclopentylacetic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.34(s，1H)，7.72(d，J＝7.6Hz，1H)，7.57-7.49(m，2H)，7.49-7.23(m，6H)，6.01(bs，1H)，4.76(s，4H)，3.90-3.74(m，1H)，2.49-2.25(m，2H)，2.20-1.99(m，3H)，1.94-1.82(m，1H)，1.68(tdd，J＝9.4，8.9，4.4Hz，2H)，1.64-1.42(m，7H)，1.31-1.01(m，2H)；MS(ESI(+))m/e444(M+H)+。
Example 1557
N- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (4-aminocyclohex-1-enyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and cyclopropylacetic acid for 4- (isoindoline-2-carboxamido) benzoic acid. 1H NMR(300MHz，DMSO-d6)δ8.36(s，1H)，7.70(d，J＝7.6Hz，1H)，7.66-7.47(m，2H)，7.47-7.24(m，6H)，6.02(bs，1H)，4.76(s，4H)，3.88-3.78(m，1H)，2.49-2.26(m，3H)，2.12-1.82(m，4H)，1.72-1.50(m，1H)，1.13-0.88(m，1H)，0.52-0.33(m，2H)，0.18-0.01(m，2H)；MS(ESI(+))m/e 416(M+H)+。
Example 1558
N- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (4-aminocyclohex-1-enyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and 2-hydroxy-2-methylpropionic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.36(s，1H)，7.52(t，J＝8.6Hz，2H)，7.46-7.39(m，1H)，7.35(tdd，J＝8.8，7.1，3.7Hz，6H)，6.07-5.96(m，1H)，5.40(s，1H)，4.77(s，4H)，3.92-3.76(m，1H)，2.46(s，1H)，2.39-2.25(m，1H)，2.24-2.09(m，2H)，1.93-1.78(m，1H)，1.70(dt，J＝12.4，7.7Hz，1H)，1.25(s，6H)；MS(ESI(+))m/e 420(M+H)+。
Example 1559
N- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (4-aminocyclohex-1-enyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and tetrahydro-2H-pyran-4-carboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.36(s，1H)，7.76(d，J＝7.6Hz，1H)，7.57-7.49(m，2H)，7.46-7.23(m，6H)，6.02(bs，1H)，4.76(s，4H)，3.91-3.75(m，4H)，3.31-3.17(m，2H)，2.43-2.26(m，2H)，2.12-1.97(m，1H)，1.93-1.81(m，1H)，1.71-1.48(m，6H)；MS(ESI(+))m/e 446(M+H)+。
Example 1560
N- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide
The title compound was prepared as described in example 1C, substituting N- (4- (4-aminocyclohex-1-enyl) phenyl) isoindoline-2-carboxamide for 3-phenylpropan-1-amine and cyclohexanecarboxylic acid for 4- (isoindoline-2-carboxamido) benzoic acid.1H NMR(300MHz，DMSO-d6)δ8.35(s，1H)，7.64(d，J＝7.6Hz，1H)，7.57-7.49(m，2H)，7.47-7.23(m，6H)，6.01(bs，1H)，4.76(s，4H)，3.84-3.54(m，1H)，2.49-2.24(m，2H)，2.20-1.93(m，2H)，1.91-1.77(m，1H)，1.78-1.48(m，6H)，1.47-1.06(m，6H)；MS(ESI(+))m/e 444(M+H)+。

Claims (20)

1. A compound of formula (Ic) and pharmaceutically acceptable salts thereof
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R2Is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R2Alkyl of (2)Alkenyl and alkynyl groups are optionally substituted with one, two, three or four groups independently selected from: r4，OR4，SR4，S(O)R4，SO2R4，C(O)R4，CO(O)R4，OC(O)R4，OC(O)OR4，NHC(O)R4，NR4C(O)R4，NHS(O)2R4，NR4S(O)2R4，NHC(O)OR4，NR4C(O)OR4，NHC(O)NH2，NHC(O)NHR4，NHC(O)N(R4)2，NR4C(O)NHR4，NR4C(O)N(R4)2，C(O)NH2，C(O)NHR4，C(O)N(R4)2，C(O)NHOH，C(O)NHOR4，C(O)NHSO2R4，C(O)NR4SO2R4，SO2NH2，SO2NHR4，SO2N(R4)2，C(O)H，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R2Optionally substituted at the para position with a group independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，CHNOR5，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3Br or I; wherein each R2Optionally substituted with one F; wherein each R2The heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r5，OR5，SR5，S(O)R5，SO2R5，C(O)R5，CO(O)R5，OC(O)R5，OC(O)OR5，NH2，NHR5，N(R5)2，NHC(O)R5，NR5C(O)R5，NHS(O)2R5，NR5S(O)2R5，NHC(O)OR5，NR5C(O)OR5，NHC(O)NH2，NHC(O)NHR5，NHC(O)N(R5)2，NR5C(O)NHR5，NR5C(O)N(R5)2，C(O)NH2，C(O)NHR5，C(O)N(R5)2，C(O)NHOH，C(O)NHOR5，C(O)NHSO2R5，C(O)NR5SO2R5，SO2NH2，SO2NHR5，SO2N(R5)2，C(O)H，C(O)OH，OH，CN，N3，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R3independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r 6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R4independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, cycloalkyl or heterocyclyl; wherein each R4Is optionally substituted with one, two, three or four groups independently selected from: r7，OR7，SR7，S(O)R7，SO2R7，C(O)R7，OC(O)R7，OC(O)OR7，NH2，NHR7，NHC(O)R7，NR7C(O)R7，NHS(O)2R7，NR7S(O)2R7，NHC(O)OR7，NR7C(O)OR7，NHC(O)NH2，NHC(O)NHR7，NHC(O)N(R7)2，NR7C(O)NHR7，NR7C(O)N(R7)2，C(O)NH2，C(O)NHR7，C(O)N(R7)2，C(O)NHOH，C(O)NHOR7，C(O)NHSO2R7，C(O)NR7SO2R7，SO2NH2，SO2NHR7，SO2N(R7)2，C(O)H，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R4The aryl and heterocyclyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r8，OR8，SR8，S(O)R8，SO2R8，C(O)R8，CO(O)R8，OC(O)R8，OC(O)OR8，NH2，NHR8，NHC(O)R8，NR8C(O)R8，NHS(O)2R8，NR8S(O)2R8，NHC(O)OR8，NR8C(O)OR8，NHC(O)NH2，NHC(O)NHR8，NHC(O)N(R8)2，NR8C(O)NHR8，NR8C(O)N(R8)2，C(O)NH2，C(O)NHR8，C(O)N(R8)2，C(O)NHOH，C(O)NHOR8，C(O)NHSO2R8，C(O)NR8SO2R8，SO2NH2，SO2NHR8，SO2N(R8)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R7independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R7Is optionally substituted with one, two, three or four groups independently selected from: r 11，OR11，SR11，S(O)R11，SO2R11，NHR11，N(R11)2，C(O)R11，C(O)NH2，C(O)NHR11，C(O)N(R11)2，NHC(O)R11，NR11C(O)R11，NHSO2R11，NHC(O)OR11，SO2NH2，SO2NHR11，SO2N(R11)2，NHC(O)NH2，NHC(O)NHR11，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R8independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12，SR12，S(O)R12，SO2R12，NHR12，N(R12)2，C(O)R12，C(O)NH2，C(O)NHR12，C(O)N(R12)2，NHC(O)R12，NR12C(O)R12，NHSO2R12，NHC(O)OR12，SO2NH2，SO2NHR12，SO2N(R12)2，NHC(O)NH2，NHC(O)NHR12，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R11independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R12independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R12The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more alkoxy groups;
wherein R is3、R5、R6、R7、R8、R9、R10、R11And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r 13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrakisHydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r 15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I; wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
R15independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted by one, two, three or four alkoxy groups；
R16Independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when X is1、X2And X3Is CH, R2When it is phenyl, R5Is not methyl;
provided that when X is1、X2And X3Is CH, R2Is being OR5When it is a substituted phenyl radical, R5Is not methyl;
provided that when R is2When it is unsubstituted alkyl or optionally substituted alkyl, R2Is C4-C6-an alkyl group;
provided that when R is 13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
2. A compound of formula (Vc) or a pharmaceutically acceptable salt thereof
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH;X2is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R5independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R5Is optionally substituted with one, two, three or four groups independently selected from: r9，OR9，SR9，S(O)R9，SO2R9，C(O)R9，CO(O)R9，OC(O)R9，OC(O)OR9，NH2，NHR9，N(R9)2，NHC(O)R9，NR9C(O)R9，NHS(O)2R9，NR9S(O)2R9，NHC(O)OR9，NR9C(O)OR9，NHC(O)NH2，NHC(O)NHR9，NHC(O)N(R9)2，NR9C(O)NHR9，NR9C(O)N(R9)2，C(O)NH2，C(O)NHR9，C(O)N(R9)2，C(O)NHOH，C(O)NHOR9，C(O)NHSO2R9，C(O)NR9SO2R9，SO2NH2，SO2NHR9，SO2N(R9)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R9independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R9Is optionally substituted with one, two, three or four groups independently selected from: alkoxy, OH, cycloalkyl, aryl or heterocyclyl;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R5、R6、R9And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R 13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl and cycloalkenyl, optionally substituted with one, two, three or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r 16，OR16OH, F, Cl, Br or I;
R15independently at each occurrence, is selected from alkyl, wherein R is15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
3. A compound of formula (VIIc) or a pharmaceutically acceptable salt thereof
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH;X2is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N;
represents a single or double bond;
R1is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
wherein R is3、R6And R10The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl,pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R 13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, tetrahydrothien-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, thienyl, and the like,Isoxazolyl, cycloalkyl, and cycloalkenyl are optionally substituted with one, two, three, or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r16，OR16OH, F, Cl, Br or I;
R15at each timeIndependently at the occurrence, is selected from alkyl, wherein R 15Is optionally substituted with one, two, three or four alkoxy groups; and
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
4. A compound of formula (VIIic) or a pharmaceutically acceptable salt thereof
Wherein
X1、X2And X3Is CH; or
X1And X3Is CH; x2Is N; or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1(ii) a Or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N；
R1Is R3，OR3，SR3，S(O)R3，SO2R3，C(O)R3，C(O)OR3，OC(O)R3，NHR3，N(R3)2，C(O)NH2，C(O)NHR3，C(O)N(R3)2，NHC(O)R3，NR3C(O)R3，NHC(O)OR3，NR3C(O)OR3，SO2NH2，SO2NHR3，SO2N(R3)2，NHSO2R3，NR3SO2R3，NHSO2NHR3，NHSO2N(R3)2，NR3SO2NHR3，NR3SO2N(R3)2，C(O)NHSO2R3，NHSO2NHR3，F，Cl，Br，I，CN，NH2，NO2，N3，OH，C(O)H，CF3C (O) OH or C (O) NH2；
R3Independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each R3Is optionally substituted with one, two, three or four groups independently selected from: r6，OR6，SR6，S(O)R6，SO2R6，C(O)R6，CO(O)R6，OC(O)R6，OC(O)OR6，NH2，NHR6，N(R6)2，NHC(O)R6，NR6C(O)R6，NHS(O)2R6，NR6S(O)2R6，NHC(O)OR6，NR6C(O)OR6，NHC(O)NH2，NHC(O)NHR6，NHC(O)N(R6)2，NR6C(O)NHR6，NR6C(O)N(R6)2，C(O)NH2，C(O)NHR6，C(O)N(R6)2，C(O)NHOH，C(O)NHOR6，C(O)NHSO2R6，C(O)NR6SO2R6，SO2NH2，SO2NHR6，SO2N(R6)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R6independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R 6Is optionally substituted with one, two, three or four groups independently selected from: r10，OR10，SR10，S(O)R10，SO2R10，NHR10，N(R10)2，C(O)R10，C(O)NH2，C(O)NHR10，C(O)N(R10)2，NHC(O)R10，NR10C(O)R10，NHSO2R10，NHC(O)OR10，SO2NH2，SO2NHR10，SO2N(R10)2，NHC(O)NH2，NHC(O)NHR10，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R8independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R8Is optionally substituted with one, two, three or four groups independently selected from: r12，OR12，SR12，S(O)R12，SO2R12，NHR12，N(R12)2，C(O)R12，C(O)NH2，C(O)NHR12，C(O)N(R12)2，NHC(O)R12，NR12C(O)R12，NHSO2R12，NHC(O)OR12，SO2NH2，SO2NHR12，SO2N(R12)2，NHC(O)NH2，NHC(O)NHR12，OH，(O)，C(O)OH，N3，CN，NH2，CF3，CF2CF3F, Cl, Br or I;
R10independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl;
R12independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R12The alkyl, alkenyl and alkynyl groups of (a) are optionally substituted with one or more alkoxy groups;
wherein R is3、R6、R8、R10And R12The cyclic moieties represented are optionally substituted with one, two, three, four, five or six groups independently selected from: r13，OR13，SR13，S(O)R13，SO2R13，C(O)R13，CO(O)R13，OC(O)R13，OC(O)OR13，NH2，NHR13，N(R13)2，NHC(O)R13，NR13C(O)R13，NHS(O)2R13，NR13S(O)2R13，NHC(O)OR13，NR13C(O)OR13，NHC(O)NH2，NHC(O)NHR13，NHC(O)N(R13)2，NR13C(O)NHR13，NR13C(O)N(R13)2，C(O)NH2，C(O)NHR13，C(O)N(R13)2，C(O)NHOH，C(O)NHOR13，C(O)NHSO2R13，C(O)NR13SO2R13，SO2NH2，SO2NHR13，SO2N(R13)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3，SCF3F, Cl, Br or I;
R13independently at each occurrence, is selected from alkyl, alkenyl, alkynyl,aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ]]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-onyl, 1, 1-tetrahydrothiophen-3-yl dioxide, tetrahydro-2H-thiopyran-3-yl 1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isoxazolyl, cycloalkyl or cycloalkenyl; wherein each R 13Is optionally substituted with one, two, three or four groups independently selected from: r14，OR14，SR14，S(O)R14，SO2R14，C(O)R14，OC(O)R14，OC(O)OR14，NH2，NHR14，N(R14)2，NHC(O)R14，NR14C(O)R14，NHS(O)2R14，NR14S(O)2R14，NHC(O)OR14，NR14C(O)OR14，NHC(O)NH2，NHC(O)NHR14，NHC(O)N(R14)2，NR14C(O)NHR14，NR14C(O)N(R14)2，C(O)NH2，C(O)NHR14，C(O)N(R14)2，C(O)NHOH，C(O)NHOR14，C(O)NHSO2R14，C(O)NR14SO2R14，SO2NH2，SO2NHR14，SO2N(R14)2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R13Aryl, tetrahydrofuryl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno [3, 2-c ] of]Pyridyl, furo [3, 2-c ]]Pyridyl, pyrrolidin-2-one, tetrahydrothiophen-3-yl-1, 1-dioxide, tetrahydro-2H-thiopyran-3-yl-1, 1-dioxide, dioxanyl, tetrahydropyranyl, piperidyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolylThienyl, furyl, morpholinyl, isoxazolyl, cycloalkyl, and cycloalkenyl are optionally substituted with one, two, three, or four groups independently selected from: r15，OR15，SR15，S(O)R15，SO2R15，C(O)R15，CO(O)R15，OC(O)R15，OC(O)OR15，NH2，NHR15，N(R15)2，NHC(O)R15，NR15C(O)R15，NHS(O)2R15，NR15S(O)2R15，NHC(O)OR15，NR15C(O)OR15，NHC(O)NH2，NHC(O)NHR15，NHC(O)N(R15)2，NR15C(O)NHR15，NR15C(O)N(R15)2，C(O)NH2，C(O)NHR15，C(O)N(R15)2，C(O)NHOH，C(O)NHOR15，C(O)NHSO2R15，C(O)NR15SO2R15，SO2NH2，SO2NHR15，SO2N(R15)2，C(O)H，C(O)OH，OH，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I;
R14independently at each occurrence, is selected from alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl or cycloalkenyl; wherein each R14Is optionally substituted with one, two, three or four groups independently selected from: heterocyclyl, alkoxy, NH2，SO2NH2，C(O)H，C(O)OH，OH，(O)，CN，N3，NO2，CF3，CF2CF3，OCF3，OCF2CF3F, Cl, Br or I; wherein each R14The aryl, heterocyclyl, cycloalkyl and cycloalkenyl groups of (a) are optionally substituted with one, two, three or four groups independently selected from: r 16，OR16OH, F, Cl, Br or I; wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
R15independently at each occurrence, is selected from alkyl; wherein R is15Is optionally substituted with one, two, three or four alkoxy groups;
R16independently at each occurrence, is selected from alkyl, wherein R is16Is optionally substituted with one, two, three or four alkoxy groups;
provided that when R is13When it is piperidinyl, it is substituted piperidinyl; and
provided that when R is13When it is pyrrolinyl, X1、X2And X3Is N.
5. A compound of claim 1, claim 2, claim 3 or claim 4, or a pharmaceutically acceptable salt thereof; wherein
X1、X2And X3Is CH, or
X1And X3Is CH; x2Is CR1(ii) a Or
X2And X3Is CH; x1Is CR1(ii) a Or
X1Is CH; x2And X3Is CR1。
6. A compound of claim 1, claim 2, claim 3 or claim 4, or a pharmaceutically acceptable salt thereof; wherein
X1And X3Is CH; x2Is N; or
X2Is CH; x1And X3Is N; or
X2And X3Is CH; x1Is N; or
X1Is CH; x2Is N; x3Is CR1(ii) a Or
X1Is CR1；X2Is N; x3Is CH; or
X1Is N; x2Is CR1；X3Is CH; or
X1Is N; x2Is CR1；X3Is N.
7. A compound of claim 1, claim 2, claim 3 or claim 4, or a pharmaceutically acceptable salt thereof; wherein
X1And X3Is CH; x2Is N.
8. A compound of claim 1 or a pharmaceutically acceptable salt thereof; wherein
R2Is at para position by R5Substituted phenyl; and
R5is phthalazin-1 (2H) -one, isoquinolinyl, isoquinolin-1 (2H) -one, 5, 6, 7, 8-tetrahydrophthalazin-1 (2H) -one, 5-fluorophthalazin-1 (2H) -one, (Z) -3H-benzo [ d ] b][1，2]Diaza derivatives-4(5H) -keto, 5- (trifluoromethyl) phthalazin-1 (2H) -keto, pyrrolo [1, 2-d][1，2，4]Triazin-1 (2H) -one or isoindolin-1-one.
9. The compound of claim 1 selected from:
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (furo [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (thieno [3, 2-c ] pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dihydro-1, 4-benzodioxin-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 3-fluoro-5- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrimidin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (2-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-methoxyphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (4-acetylphenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 3-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (6-aminohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-benzodioxol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (pyridazin-3-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (3-fluorophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dihydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-propoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-cyanophenyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-hydroxy-2-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methyl-1H-indazol-5-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 5- ({4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } amino) -1H-indazole-3-carboxylate;
n- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (5-chloropyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1, 4-benzodioxin-6-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-fluorobenzoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methoxy-1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-propoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (pyridin-4-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (dimethylamino) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoro-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 3-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1, 3-benzodioxol-5-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (4-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- {4- [ (2-phenoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-hydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({1- [ (3S) -tetrahydrofuran-3-yl ] -1H-pyrazol-4-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 4-dioxa-8-azaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (2, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylthio) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (trifluoromethyl) thio ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (2-fluorophenyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (1H-imidazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (hydroxymethyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-benzodioxol-5-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-isopropyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiomorpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzylpiperidin-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-acetylamino-2-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [3- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-imidazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1R) -1- (3-cyanophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (2-hydroxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyanomethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclohexylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (3, 4-dihydroisoquinolin-2 (1H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1H-indol-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (phenylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (diethylamino) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-phenylethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-aminophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } piperidin-4-yl) carbamate;
N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ 3-chloro-5- (trifluoromethyl) pyridin-2-yl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (cyclohexylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-chlorobenzyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (diethylcarbamoyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-hydroxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-6-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (5, 6-dihydro [1, 2, 4] triazolo [4, 3-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-fluoropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylmethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3, 4, 9-tetrahydro-2H- β -carbolin-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tert-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [4- (trifluoromethyl) phenyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3, 3-difluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-benzylpyrrolidin-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-carbamoylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopropylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (methylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (pent-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dioxolan-2-ylmethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (4-fluorophenyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-hydroxy-2-methylprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-phenyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (sec-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ bis (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ butyl (ethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isobutyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4-carbamoylphenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (trifluoromethyl) pyrrolidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ ethyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 6-dimethylmorpholin-4-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethylpyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (prop-2-yn-1-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ isopropyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyanoethyl) (cyclopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ ethyl (isopropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoropyrrolidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -N-isopropyl- β -alanine;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5, 6-dimethoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-chlorophenoxy) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenyl-1, 3-thiazol-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid;
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (aminomethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (2-hydroxy-2-methylpropanoyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetylamino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (N, N-dimethylglycyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methoxyacetyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methylsulfonyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4, 4, 4-trifluorobutanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpentanoyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (benzyloxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ N- (2-furoyl) glycyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [4- (2-thienyl) butyryl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-oxo-4-phenylbutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (N-benzoylglycyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenoxybutyryl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (propionylamino) phenyl ] -amide;
n- [4- (pentanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (heptanoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-4-enoylamino) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopropylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (4-methylpiperazin-1-yl) propionyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylate;
2- ({4- [ (cyclopentylacetyl) amino ] phenyl } carbamoyl) isoindoline-5-carboxylic acid;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-cyclopentylethyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester;
n- [4- (1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-methyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1E) -5-phenylpent-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-hydroxyethyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (1-propyl-1H-pyrazol-4-yl) pyridin-3-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-phenylpentyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [ 2-fluoro-4- (1-propyl-1H-pyrazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 2-fluoro-4- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (isopropylsulfonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-benzoylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (isopropylsulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (benzenesulfonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (benzoylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [3- (butyrylamino) pyrrolidin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperazine-1-carboxylic acid tert-butyl ester;
n- [4- (4-propionylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopropylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-butanoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-isobutyryl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (2-benzoyl-2, 3-dihydro-1H-isoindol-5-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [2- (3-methylbutyl) -2, 3-dihydro-1H-isoindol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexyloxy) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (4-chlorophenoxy) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (piperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n, N' -hexane-1, 6-diylbis (1, 3-dihydro-2H-isoindole-2-carboxylic acid amide);
n- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
ethyl 6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] hexanoate;
n-hexyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n-octyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (1-methyl-1H-pyrazol-4-yl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [6- (methylamino) -6-oxohexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 6-oxo-6- [ (3-phenylpropyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (3-methylbutyl) amino ] -6-oxohexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (5- { [4- (pyridin-2-yl) piperazin-1-yl ] carbonyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-phenylpropyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-phenylpropyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] -1, 3-thiazol-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4, 5, 6, 7, 8-hexahydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (8-fluoro-4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (morpholin-4-ylmethyl) -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-4, 5-dihydro-3H-2, 3-benzodiazepine-1-yl) phenyl]-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (4-methylpiperazin-1-yl) methyl ] -N- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (dimethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (diethylamino) methyl ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ 4-oxo-8- (trifluoromethyl) -3, 4-dihydrophthalazin-1-yl ] phenyl } -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (1-methylpiperidin-4-yl) oxy ] -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3R) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- { [ (3S) -3-fluoropyrrolidin-1-yl ] methyl } -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (azetidin-1-ylmethyl) -N- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxo-1, 2-dihydropyrrolo [1, 2-d ] [1, 2, 4] triazin-4-yl) phenyl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperidine-1-carboxylic acid tert-butyl ester;
n- [4- (5-propyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (piperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [5- (3-methylbutyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (5-benzyl-1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-chloropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-oxopyrrolidin-1-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxy-2, 3-dihydro-1H-inden-1-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-hydroxycyclopropyl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {6- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] -1H-benzimidazol-2-yl } piperazine-1-carboxylic acid tert-butyl ester;
n- [2- (piperazin-1-yl) -1H-benzoimidazol-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-benzoylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (tetrahydrofuran-3-yl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
N- (4- { [ (3-phenylpropyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- {4- [1- (4-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (tetrahydrofuran-3-ylmethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2S) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2R) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-phenylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-methoxyethyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2- (2-hydroxyethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-3-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-4-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- (2-methoxyethyl) -N2- {4- [ (propylamino) carbonyl group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- (4-cyanophenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (trifluoromethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (tetrahydrofuran-3-ylmethyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-pyridin-2-ylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (1, 2-dihydroxyethyl) -N- {4- [ (propylamino) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (1 '-butyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and
n- [2- (4-acetylpiperazin-1-yl) -1H-benzimidazol-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-D-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (ethoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (3-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-chlorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [3- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-furoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-thienylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (1H-pyrrol-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2, 5-dimethyl-1H-pyrrol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 3-thiazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3, 5-dimethyl-1, 2-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isonicotinoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridazin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrimidin-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- (4- {1- [3- (piperidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [6- (benzoylamino) hexyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (benzoylamino) methyl ] benzyl } carbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-L-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (5-oxo-D-prolyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {4- [ (1-acetylpiperidin-4-yl) carbonyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-acetamidobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (methylsulfonyl) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-butyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isobutyrylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-methylbutyryl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 3, 3-trifluoropropionyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (methoxyacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (tetrahydrofuran-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclopentylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (cyclohexylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (2-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-methoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-chlorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-cyanobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [3- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [4- (dimethylamino) benzoyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3, 4-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (3, 5-dimethoxybenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (3, 4-dimethoxyphenyl) acetyl ] piperazin-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (3-furoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrrol-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1H-pyrazol-5-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-isonicotinyl piperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyridazin-3-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrazin-2-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (pyrimidin-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [4- (N, N-dimethyl- β -alanyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-acetylpiperazin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (2-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (4-fluorobenzoyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (phenylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (1, 3-thiazol-4-ylcarbonyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [4- (morpholin-4-ylacetyl) piperazin-1-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxo-2, 3-dihydro-1H-isoindol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (1-oxo-1, 2-dihydroisoquinolin-4-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-oxo-3, 4-dihydrophthalazin-1-yl) cyclohex-3-en-1-yl ] -5- (pyrrolidin-1-ylmethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1- (2-phenylethyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- [2- (dimethylamino) ethyl group]-N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (morpholin-4-ylcarbonyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { benzyl [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutoxycarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
methyl 4- { [ (5-cyano-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoate;
n- (4- { (E) - [ (benzyloxy) imino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-aminopyrrolidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-methylbutyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-phenylpropyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- [4- ({ benzyl [3- (morpholin-4-yl) propyl ] amino } methyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-methyl-1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-methoxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
N2- {4- [ (cyclopentylacetyl) amino group]Phenyl } -N5- (2-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (aminomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4- (methylthio) but-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3S) -1-hydroxy-3-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3R) -1, 3-dihydroxybutan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -1-hydroxyhex-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypentan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2R) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-cyclohexyl-3-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ (2R) -1-hydroxy-3- [ (4-methylbenzyl) thio ] propan-2-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-tert-butylphenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methoxy-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [6- (benzoylamino) hexyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (pyridin-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (2-methoxyethoxy) acetyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4-phenylbutyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [1- (3-methylbutyl) -1H-pyrazol-4-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [ (3-methylbutyl) carbamoyl ] pyrazin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6-acetamidohexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (1E) -3- [ benzyl (methyl) amino ] prop-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (4-phenoxypiperidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3-phenoxyazetidin-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ benzyl (methyl) amino ] methyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxypiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-hydroxy-2-methylpropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5, 6-dihydroimidazo [1, 5-a ] pyrazin-7 (8H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbutyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [2- (2-oxopyrrolidin-1-yl) ethyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1-benzylpiperidin-4-yl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-phenylpropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (morpholin-4-yl) benzyl ] -1H-1, 2, 3-triazol-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1-isobutyl-1H-1, 2, 3-triazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylmethyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxypropyl) -1H-1, 2, 3-triazol-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] pyridin-2-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- (4- { [ (2-methoxyethoxy) acetyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (1 '-isobutyryl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (1 '-benzoyl-1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [1 '- (tetrahydrofuran-3-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {1 '- [ (2-methoxyethoxy) acetyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [4- (methylsulfonyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (ethoxyacetyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (cyclopentylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-hydroxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-methoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (2-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-fluorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-chlorobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (3-cyanobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (4-cyanobenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [3- (dimethylamino) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [4- (dimethylamino) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [3- (trifluoromethyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [4- (trifluoromethyl) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [3- (trifluoromethoxy) benzoyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 3-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 4-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (2, 5-dimethoxybenzoyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (phenylacetyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (3-fluorophenyl) acetyl ] amino } hexyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- {4- [ (morpholin-4-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (morpholin-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [6- (benzoylamino) hexyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
4-fluoro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {6- [ (pyridin-3-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {6- [ (pyridin-2-ylcarbonyl) amino ] hexyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (2-hydroxy-2-methylpropionyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {1 '- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (7-oxo-7- { [ (3R) -tetrahydrofuran-3-ylmethyl ] amino } heptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- { 7-oxo-7- [ (tetrahydro-2H-pyran-4-ylmethyl) amino ] heptyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (azetidin-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (trifluoromethyl) piperidin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [5- (morpholin-4-ylmethyl) -1, 2, 4-oxadiazol-3-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {5- [ (4-methylpiperazin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5- { [ (3-methylbutyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-hydroxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-chlorobenzoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [1 ' - (2-hydroxy-2-methylpropanoyl) -1 ', 2 ', 3 ', 6 ' -tetrahydro-2, 4 ' -bipyridin-5-yl ] -1, 3 ' -dihydro-2H-isoindole;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydrofuran-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (tetrahydro-2H-pyran-4-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (1, 4-dioxan-2-ylcarbonyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {1 '- [ (1, 1-tetrahydrothiophen-3-yl dioxide) carbonyl ] -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [1 ' - (2-hydroxy-2-methylpropanoyl) -1 ', 2 ', 3 ', 6 ' -tetrahydro-3, 4 ' -bipyridin-6-yl ] -1, 3 ' -dihydro-2H-isoindole;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (2-aminoethyl) -1H-imidazol-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2, 2-dimethyl-1, 3-dioxolan-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-methoxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4S) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4R) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } -2-oxoethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3- { benzyl [3- (morpholin-4-yl) propyl ] amino } -3-oxopropyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-cyano-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-chloro-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (6-bromo-2-oxoquinolin-1 (2H) -yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [6- (3-acetylphenyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [1 '- (morpholin-4-ylacetyl) -1', 2 ', 3', 6 '-tetrahydro-2, 4' -bipyridin-5-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [1 '- (morpholin-4-ylacetyl) -1', 2 ', 3', 6 '-tetrahydro-3, 4' -bipyridin-6-yl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (2- { (4-fluorobenzyl) [4- (pyridin-3-yl) benzyl ] amino } -1, 3-thiazol-5-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2-benzyl-1, 3-thiazol-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (7- { benzyl [3- (morpholin-4-yl) propyl ] amino } -7-oxoheptyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-thiazol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (4-methylphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-dihydroxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (2-furoyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (tetrahydrofuran-2-ylcarbonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [4- (ethanesulfonyl) piperazin-1-yl ] carbonyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2, 3-dihydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1-hydroxy-4-methylpent-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (5- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } pyridin-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.3] hept-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 6-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.4] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (3, 9-diazaspiro [5.5] undecan-3-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { benzyl [3- (morpholin-4-yl) propyl ] amino } -4-oxobutyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4-phenylbutyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2- { benzyl [3- (morpholin-4-yl) propyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetyl-N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (1-hydroxyethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butyrylamino) phenyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -pyrrolidin-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methoxybenzyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [3.4] oct-6-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 7-diazaspiro [4.4] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 6-diazaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (2-oxa-7-azaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [6- (3-acetylphenyl) -4- (3-hydroxypropyl) -2-oxoquinolin-1 (2H) -yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5- (acetamidomethyl) -N- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {5- [2- (2-chlorobenzyl) -1, 3-thiazol-4-yl ] -2-thienyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4-fluorophenyl) butyl ] -5- (hydroxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (3R) -1-isobutyrylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-benzoylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (methylsulfonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-isobutyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylmethyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (2-hydroxypropan-2-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
{4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzyl } carbamic acid tert-butyl ester;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylacetyl) amino ] phenyl } -5- (methoxymethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (5- { [ (tetrahydrofuran-2-ylmethyl) amino ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {5- [ (4-methoxypiperidin-1-yl) methyl ] -1, 2, 4-oxadiazol-3-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- [4- (5- { [4- (2-methoxyethyl) piperazin-1-yl ] methyl } -1, 2, 4-oxadiazol-3-yl) phenyl ] -1, 3-dihydro-2H-isoindole;
n- [4- ({ [1- (morpholin-4-yl) cyclopentyl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-pentanoylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-4-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (1-acetylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {6- [ (1-isobutyrylpiperidin-4-yl) oxy ] pyridin-3-yl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] oxy ] pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (methoxyacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopropylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopropylacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclobutylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopentylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [1- (cyclopentylacetyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (6- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } pyridin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
tert-butyl (2- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } ethyl) carbamate;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) sulfamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-phenylpropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (phenylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxyphenyl) acetyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-benzoylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-ethoxypropionyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (1-methylcyclopropyl) carbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-acetylpyrrolidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (4, 4, 4-trifluorobutanoyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethoxyacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpiperidin-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
Tert-butyl [ (1- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } azetidin-3-yl) methyl ] carbamate;
n- (4- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (morpholin-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (2, 3-dimethylbutyryl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (cyclohexylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclohexylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tricyclo [ 3.3.1.1-3, 7- ] decan-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methoxycyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [4- (acetylamino) phenyl ] sulfonyl } amino) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (propylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-propylphenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (butanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ ({ [ (1S, 4R) -7, 7-dimethyl-2-oxobicyclo [2.2.1] hept-1-yl ] methyl } sulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethanesulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (benzylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-fluorophenyl) sulfonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (thiophen-2-ylsulfonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [4.4] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 6-diazaspiro [4.5] decan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 7-diazaspiro [4.5] decan-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (2, 9-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 8-diazaspiro [5.5] undecan-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [5.5] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.6] undecan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-oxa-4, 8-diazaspiro [5.5] undecan-4-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 8-diazaspiro [4.5] decan-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1, 8-diazaspiro [4.5] decan-8-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 7-diazaspiro [3.5] non-7-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1, 6-diazaspiro [3.5] non-1-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (2, 5-diazaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (5-oxa-2-azaspiro [3.4] oct-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (6-oxa-2-azaspiro [3.5] non-2-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydro-5H-furo [2, 3-c ] pyrrol-5-ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (tetrahydro-1H-furo [3, 4-c ] pyrrol-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (hexahydrofuro [3, 4-c ] pyridin-5 (3H) -ylcarbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydro-2H-pyran-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (N, N-dimethylglycyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (4, 4-difluorocyclohexyl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (piperidin-1-ylsulfonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [1- (1, 3-thiazol-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -D-phenylpropanamide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -L-phenylpropanamide;
N- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (5-methyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-chloro-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({4- [2- (2-hydroxyethoxy) ethyl ] piperazin-1-yl } carbonyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-carbamoylbenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ bis (2-methoxyethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (pyrazin-2-yl) piperazin-1-yl ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n2(Nalpha) - {4- [ (5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridin-6-ylcarbonyl) amino ] benzoyl } -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (4-cyclohexylpiperazin-1-yl) carbonyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- [4- (4, 5, 6, 7-tetrahydro-1H-indazol-5-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ benzyl (methyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-1-oxobutan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxyprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -1-cyanobutan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (3-methylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanocyclopropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (4-methyl-1, 3-thiazol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- [4- (butylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxyethyl) (methyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ methyl (propyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
1- {4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } azetidine-3-carboxylic acid methyl ester;
n- (4- {3- [ (3-methylbutyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (benzylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [3- (cyclopentylcarbamoyl) azetidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (cyclopentylmethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (2-methoxyethyl) carbamoyl ] azetidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopentylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrrolidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [ (dimethylamino) methyl ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (1, 3-oxazol-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) (3-methylbutyryl) amino ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (9-chloro-5-oxo-2, 3, 3a, 4, 4a, 5-hexahydro-6H-furo [2 ', 3': 2, 3] cyclobuta [1, 2-c ] quinolin-6-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ 7-chloro-1- (2-hydroxyethyl) -3-oxo-1, 3-dihydrocyclobuta (cyclobuta) [ c ] quinolin-4 (2H) -yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (1-acetylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-butyrylpiperidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (methoxyacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyryl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3, 3-trifluoropropionyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclobutylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (cyclopentylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-2-ylcarbonyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydro-2H-pyran-4-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylacetyl) piperidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (3, 5-dimethyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-difluoroethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -L-phenylalanine amide;
n- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiophen-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pyrimidin-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (5-oxo-L-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4, 4-difluorocyclohexyl) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (propan-2-yloxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-ethoxypropionyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-acetylpiperidin-4-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (ethoxyacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { 7-oxo-7- [ (3-phenylpropyl) amino ] heptyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (bicyclo [2.2.1] hept-2-ylacetyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1, 3-thiazol-5-ylcarbonyl) amino ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (4-oxo-4, 5, 6, 7-tetrahydro-1-benzofuran-3-yl) carbonyl ] amino } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {2- [ (3-methylbutyryl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (4-methylpentanoyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (ethoxyacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2- { [ (2-methoxyethoxy) acetyl ] amino } ethyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-2-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (cyclopentylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [2- (benzoylamino) ethyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {2- [ (tetrahydrofuran-3-ylacetyl) amino ] ethyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-L-prolyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-propionylazetidin-3-yl) oxy ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylbutyryl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pent-4-ynoyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (furan-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (thiophen-3-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethylglycyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (N, N-dimethyl- β -alanyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrrolidin-1-ylacetyl) azetidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (pyrrolidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({1- [3- (piperidin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-methylpiperazin-1-yl) acetyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopropylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-cyclopentylethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-3-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (3, 3-dimethylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclohexylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (3-methylbutyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopentylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (tetrahydrofuran-2-ylmethyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-methylpropyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (butanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (cyclopropylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (benzenesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4-fluorophenyl) sulfonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (ethanesulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propan-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (benzylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (propylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (thien-2-ylsulfonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -2-methylbutyryl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (4, 4-difluorocyclohexyl) carbonyl ] azetidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (5-oxo-D-prolyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2, 2-dimethylpropionyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [1- (2-methylpentanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (2-ethylbutanoyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1H-pyrrol-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (1, 2-oxazol-5-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyridazin-3-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrazin-2-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (pyrimidin-4-ylcarbonyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [ (5-methylpyrazin-2-yl) carbonyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({1- [3- (piperidin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [1- (morpholin-4-ylacetyl) piperidin-4-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({1- [3- (4-methylpiperazin-1-yl) propionyl ] piperidin-4-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
trans-3- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] cyclobutanecarboxylic acid benzyl ester;
n- [4- (4- { [ (4-methylpiperazin-1-yl) acetyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (benzoylamino) cyclohex-1-en-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (4- { [ (1-methylpiperidin-4-yl) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (1, 1-tetrahydro-2H-thiopyran-4-yl-dioxide) carbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3R) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (3S) -tetrahydrofuran-3-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (4- { [ (2S) -2-methylbutyryl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {3- [ (3-methylbutyryl) amino ] oxetan-3-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
4- ({4- [ (1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridin-2-ylcarbonyl) amino ] phenyl } sulfonyl) piperidine-1-carboxylic acid tert-butyl ester;
n- {4- [4- (propylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methoxyethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {4- [ (cyclopentylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (1, 4-dioxan-2-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopentylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (morpholin-4-ylcarbonyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [4- (cyclopropylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] piperidin-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [4- (but-2-ylcarbamoyl) piperidin-1-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-dioxido-tetrahydro-2H-thiopyran-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { (4R) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { (4S) -4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylazetidin-3-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [ trans-3- (benzylcarbamoyl) cyclobutyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { trans-3- [ (2-phenylethyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- { trans-3- [ (3-phenylpropyl) carbamoyl ] cyclobutyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methyl-1, 3-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (furan-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -3- (furan-2-yl) prop-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 3-oxazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (3, 3, 3-trifluoropropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 5-dimethyl-1H-pyrazol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methoxycyclohexyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 3-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-difluorocyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1H-pyrazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tert-butoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-1, 2, 4-triazol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (3-ethoxypropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-hydroxy-3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-pyrrol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methylpropoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1-methyl prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-hydroxycyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c1 pyridine-2-carboxamide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1- { [1- (methoxymethyl) cyclopropyl ] carbonyl } -1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (methylsulfonyl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-acetyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -4-methylpent-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-methoxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopent-1-en-1-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (thiophen-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1-methyl-1H-pyrrol-2-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (methoxyacetyl) -12, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (4-methylhexanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-dimethylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-5-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclobutylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (piperidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [2- (pyrrolidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2-methoxyethoxy) acetyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cis-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (trans-4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohexyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (6- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3R) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3R) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (3-methylbutyryl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclobutylcarbonyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ (3S) -1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({ (3S) -1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] pyrrolidin-3-yl } oxy) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3S) -1- (cyclopropylacetyl) pyrrolidin-3-yl ] oxy } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (6- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } pyridazin-3-yl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (cyclopentylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {6- [ (bicyclo [2.2.1] hept-2-ylmethyl) carbamoyl ] pyridazin-3-yl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (2-methylpropanoyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { cis-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclohexylcarbonyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { trans-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { cis-4- [ (cyclopropylacetyl) amino ] cyclohexyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {4- [ (2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2R) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (4- { [ (2S) -tetrahydrofuran-2-ylcarbonyl ] amino } cyclohex-1-en-1-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopentylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclopropylacetyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (2-hydroxy-2-methylpropanoyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {4- [ (tetrahydro-2H-pyran-4-ylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {4- [ (cyclohexylcarbonyl) amino ] cyclohex-1-en-1-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and pharmaceutically acceptable salts thereof.
10. The compound of claim 1 selected from:
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
11. The compound of claim 1 selected from:
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
12. The compound of claim 2 selected from:
N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (aminomethyl) benzyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dihydro-1, 4-benzodioxin-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5-methyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 3-fluoro-5- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-nitro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 3-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-methylbutyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (6-aminohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-thienyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1, 3-benzodioxol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (benzylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dihydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-propoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxy-2-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methyl-1H-indazol-5-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
Methyl 5- ({4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } amino) -1H-indazole-3-carboxylate;
n- (4- { [2- (2-oxopyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethyl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (2, 3-dihydro-1, 4-benzodioxin-6-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (5-methoxy-1H-indol-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2R) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-propoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4, 5-trimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methylpiperidin-1-yl) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (dimethylamino) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (trifluoromethoxy) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluoro-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 3-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (2-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1, 3-benzodioxol-5-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4-chloro-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2- [4- (Propylcarbamoyl) phenyl]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- {4- [ (2-phenoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-hydroxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-fluorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({1- [ (3S) -tetrahydrofuran-3-yl ] -1H-pyrazol-4-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylthio) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-ethoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (trifluoromethyl) thio ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 4-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (1H-imidazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -5- (trifluoromethyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (hydroxymethyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-benzodioxol-5-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (1-isopropyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-ethyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 5-dimethoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-benzylpiperidin-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-acetylamino-2-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [3- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-imidazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1- (3-cyanophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-cyanophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-chlorophenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (cyanomethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclohexylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-hydroxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (phenylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (diethylamino) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-aminophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3-chlorobenzyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-hydroxy-6-methylphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-fluoropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tert-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methylbut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-benzylpyrrolidin-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-fluorophenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (cyclopropylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (methylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pent-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (4-fluorophenyl) -1H-pyrazol-4-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-hydroxy-2-methylprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-phenyl-1H-pyrazol-4-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [4- (trifluoromethyl) phenyl ] ethyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (sec-butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (prop-2-yn-1-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5, 6-dimethoxy-N- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (4-chlorophenoxy) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (trifluoromethoxy) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4-phenyl-1, 3-thiazol-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid methyl ester;
2- { [4- (propylcarbamoyl) phenyl ] carbamoyl } isoindoline-5-carboxylic acid;
5-amino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (hydroxymethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (aminomethyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (2-hydroxy-2-methylpropanoyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-acetylamino-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (N, N-dimethylglycyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-3-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5- (1H-pyrazol-4-yl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methoxyacetyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- [ (methylsulfonyl) amino ] -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-bromo-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 5-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-chlorobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-phenylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (5-chloropyridin-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-hydroxy-4-methoxyphenyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 4-dimethoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (2-oxopyrrolidin-1-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxy-2, 3-dihydro-1H-inden-1-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-hydroxycyclopropyl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (propylcarbamoyl) phenyl ] -5-vinyl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
n- (4- { [ (3-phenylpropyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-d ] pyrimidine-6-carboxamide;
5-fluoro-N- [4- ({ [ (2S) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- ({ [ (2R) -tetrahydrofuran-2-ylmethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (1S) -2-hydroxy-1-phenylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-3-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (propylamino) carbonyl ] phenyl } -5-pyridin-4-yl-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N5- (2-methoxyethyl) -N2- {4- [ (propylamino) carbonyl group]Phenyl } -1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (3-methylbutyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (tetrahydrofuran-3-ylmethyl) amino ] carbonyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- ({ [ (1S) -2-hydroxy-1-pyridin-2-ylethyl ] amino } carbonyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5- (1, 2-dihydroxyethyl) -N- {4- [ (propylamino) carbonyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [6- (benzoylamino) hexyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({4- [ (benzoylamino) methyl ] benzyl } carbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N5- [2- (dimethylamino) ethyl group]-N2- [4- (Propylcarbamoyl) phenyl ]-1, 3-dihydro-2H-isoindole-2, 5-dicarboxamide;
5- (morpholin-4-ylcarbonyl) -N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (isobutoxycarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxy-4- (methylthio) but-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3S) -1-hydroxy-3-methylpent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2S) -1-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S, 3R) -1, 3-dihydroxybutan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxyhex-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-hydroxypentan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2S) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S, 2R) -2-hydroxycyclopentyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-cyclohexyl-3-hydroxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ (2R) -1-hydroxy-3- [ (4-methylbenzyl) thio ] propan-2-yl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (4-tert-butylphenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methoxy-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-methyl-N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- [4- (propylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-hydroxy-4-methylpent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5- (hydroxymethyl) -N- {4- [ (3-methylbutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- (4- { [ (3R) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (1-hydroxy-2-methylpropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (2-oxopyrrolidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (3S) -tetrahydrofuran-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-isopropoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (isobutylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-thienylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isopropoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-isobutoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrimidin-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (pyridin-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (2, 2-dimethyl-1, 3-dioxolan-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-methoxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4S) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (4R) -2, 2-dimethyl-1, 3-dioxolan-4-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3-methyloxetan-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-thiazol-5-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -3-hydroxy-1-phenylpropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (4-methylphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1, 3-dihydroxypropan-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -1-hydroxy-3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1S) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (4-hydroxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -2-hydroxypropyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (3-furylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2R) -tetrahydrofuran-2-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydrofuran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1R) -2-hydroxy-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (2S) -1-hydroxybut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (2, 3-dihydroxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-4-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ 2-hydroxy-1- (pyridin-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (1-hydroxy-4-methylpent-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1, 1-tetrahydrothiophen-3-yl-dioxide) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (pyrrolidin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- { [ (3S) -pyrrolidin-3-ylmethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpyrrolidin-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1-methylpiperidin-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({ [ (3R) -1-isobutyrylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [ (3R) -1-benzoylpyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (tetrahydrofuran-3-ylcarbonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [1- (methylsulfonyl) pyrrolidin-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- ({ [1- (morpholin-4-yl) cyclopentyl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (4-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- ({ [3- (hydroxymethyl) oxetan-3-yl ] methyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- { [ (1S) -1- (-fluorophenyl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -2-hydroxy-1- (4-methoxyphenyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1- (1, 3-benzodioxol-5-yl) -2-hydroxyethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-oxa-8-azaspiro [4.5] decan-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- [4- (1-oxa-8-azaspiro [4.5] decan-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [ (2-oxa-9-azaspiro [5.5] undecan-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-fluoro-N- (4- { [1- (1, 3-thiazol-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -D-phenylpropanamide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - (4- { [ (5-fluoro-1, 3-dihydro-2H-isoindol-2-yl) carbonyl ] amino } benzoyl) -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [3- (5-methyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-chloro-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [3- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-carbamoylbenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (3, 4-dimethoxyphenyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N2(Nalpha) - {4- [ (5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridin-6-ylcarbonyl) amino ] benzoyl } -L-phenylpropanamide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-methoxybenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (4-methylpiperazin-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (morpholin-4-yl) benzyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [3- (piperidin-1-yl) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (4, 5, 6, 7-tetrahydro-1H-indazol-5-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
5-fluoro-N- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2R) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (pyridin-3-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -1-amino-1-oxobutan-2-yl ] carbamoyl } phenyl) -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (1-methoxyprop-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-methoxyethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (cyclopentylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (butylcarbamoyl) phenyl ] -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5-fluoro-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-fluoro-N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethylbutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (3-methyl-1, 2-oxazol-5-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -1-cyanobutan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [4- (dimethylamino) butyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (4-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (6-methoxypyridin-3-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanocyclopropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (4-methyl-1, 3-thiazol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-hydroxypropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (thiophen-2-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (4-methoxybutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2S) -1-methoxypropan-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (1-methyl-1H-pyrrol-2-yl) methyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (prop-2-yloxy) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- (4- { [3- (dimethylamino) propyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-methoxypropan-2-yl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-aminobenzyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (tetrahydro-2H-pyran-3-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-hydroxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- [4- (butylcarbamoyl) phenyl ] -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (1-cyanoethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
N- {4- [ (3R) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopentylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (cyclopropylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (pyridin-4-ylmethyl) carbamoyl ] phenyl } -5, 7-dihydro-6H-pyrrolo [3, 4-b ] pyridine-6-carboxamide;
n- {4- [ (3-methoxy-2, 2-dimethylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (4, 4-difluorocyclohexyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-cyanobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxybutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (ethylamino) -1-oxoprop-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [ (1R) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1S) -1-cyclopropylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3S) -tetrahydrofuran-3-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (tetrahydro-2H-pyran-3-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 3-oxazol-2-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- ({2- [ (dimethylamino) methyl ] benzyl } carbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1R) -2-amino-2-oxo-1-phenylethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1, 3-oxazol-2-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (2, 6-dimethylmorpholin-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro
-2H-isoindole-2-carboxamide;
n- (4- { [1- (1-methylcyclopropyl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (furan-2-yl) -2- (pyrrolidin-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (3, 5-dimethyl-1H-pyrazol-1-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (3S) -1-methyl-2-oxoazepan-3-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1, 3-thiazol-2-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (furan-2-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (1-methyl-1H-pyrazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -1-amino-4-methyl-1-oxopent-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [1- (3, 5-dimethyl-1H-pyrazol-1-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2, 2-difluoroethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (tetrahydro-2H-pyran-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (tetrahydrofuran-2-ylmethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-methoxy-2-methylpropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (5-methyl-1, 2-oxazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-4-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3, 5-dimethyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n2(Nalpha) - {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] benzoyl } -L-phenylalanine amide;
n- (4- { [2- (2-methyl-1, 3-thiazol-4-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3, 3-dimethyl-1- (methylamino) -1-oxobut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (thiophen-3-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- { [2- (5-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (3-methyl-1H-pyrazol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2S) -but-2-ylcarbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3, 3-dimethyl-2-oxobutyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (1-methyl-1H-pyrazol-3-yl) methyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (acetylamino) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (1-methoxybut-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (tetrahydro-2H-pyran-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (pyrimidin-4-ylcarbamoyl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [2- (1H-pyrrol-1-yl) ethyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -2-methylbutyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [ (1-amino-1-oxohex-2-yl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-amino-2-oxo-1-phenylethyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (3-tert-butoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [3- (methylcarbamoyl) phenyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2R) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ (2S) -3-methylbut-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-1- (morpholin-4-yl) propan-2-yl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- { [ 2-methyl-2- (morpholin-4-yl) propyl ] carbamoyl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [ (2-ethoxypropyl) carbamoyl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide; and pharmaceutically acceptable salts thereof.
13. A compound of claim 3 selected from:
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } -3, 6-dihydropyridine-1 (2H) -carboxylic acid tert-butyl ester;
N- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
4- {4- [ (1, 3-dihydro-2H-isoindol-2-ylcarbonyl) amino ] phenyl } piperidine-1-carboxylic acid tert-butyl ester;
n- [4- (1-butyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (5-oxo-D-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (ethoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methylbenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (2-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-methoxybenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (3-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-fluorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (4-chlorobenzoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [3- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [4- (dimethylamino) benzoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (3-thienylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrrol-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2, 5-dimethyl-1H-pyrrol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 3-thiazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1H-pyrazol-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3, 5-dimethyl-1, 2-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-isonicotinoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (pyridazin-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyrimidin-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
1, 3-dihydro-2H-isoindole-2-carboxylic acid amide, N- (4- {1- [3- (piperidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-butyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyryl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-benzoyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-isobutyrylpiperidin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2-hydroxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (1, 4-dioxane-2-ylcarbonyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpyrrolidin-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl) carbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (morpholin-4-ylacetyl) piperidin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1-methylpiperidin-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydro-2H-thiopyran-4-yl) -carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (N, N-dimethylglycyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methylpiperazin-1-yl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopentylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydro-2H-pyran-2-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrrolidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (pyrazin-2-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
5-cyano-N- {4- [1- (tetrahydrofuran-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (tetrahydro-2H-pyran-4-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (2-hydroxy-2-methylpropanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
5-cyano-N- {4- [1- (morpholin-4-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (3S) -tetrahydrofuran-3-ylcarbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (1, 1-dioxido-tetrahydro-2H-thiopyran-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- (4- {1- [ (3R) -tetrahydrofuran-3-ylcarbonyl ] piperidin-4-yl } phenyl) -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- (4- {1- [ (2-methyl-1, 3-oxazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (furan-3-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -3- (furan-2-yl) prop-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1, 3-oxazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3, 3, 3-trifluoropropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 5-dimethyl-1H-pyrazol-3-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4-methoxycyclohexyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2, 3-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-difluorocyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1H-pyrazol-5-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tert-butoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-1, 2, 4-triazol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-ethoxypropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (3-hydroxy-3-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [3- (1H-pyrrol-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (1-methylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methylpropoxy) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (1-methyl prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-hydroxy-2-methylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-hydroxycyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopentylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1- { [1- (methoxymethyl) cyclopropyl ] carbonyl } -1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- (4- {1- [ (methylsulfonyl) acetyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-acetyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-ethylbutanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (5-oxo-L-prolyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2E) -4-methylpent-2-enoyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-methoxy-2-methylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (cyclopent-1-en-1-ylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (thiophen-3-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- [4- (1-propionyl-1, 2, 3, 6-tetrahydropyridin-4-yl) phenyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylbutyryl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1-methyl-1H-pyrrol-2-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (methoxyacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2, 2-dimethylpropionyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (4-methylhexanoyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2, 2-dimethylcyclopropyl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-5-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclobutylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (piperidin-1-ylacetyl) -1, 2, 3, 6-tetrahydropyridin-4-yl ] phenyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [2- (pyrrolidin-1-yl) propionyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 3-dimethyl-1H-pyrazol-4-yl) carbonyl ] -1, 2, 3, 6-tetrahydropyridin-4-yl } phenyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
14. The compound of claim 4 selected from:
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
N- {4- [1- (pyridin-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -5-cyano-1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- {4- [1- (pyridin-2-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-isoindole-2-carboxylic acid amide;
n- [4- (1-benzoylpiperidin-4-yl) butyl ] -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (2-chlorobenzoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-2-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (1, 1-tetrahydrothiophen-3-yl-dioxide) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclohexylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (4, 4-difluorocyclohexyl) carbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
N- {4- [1- (2-hydroxy-2-methylpropanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2R) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2S) -tetrahydrofuran-2-ylcarbonyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (2-methoxyethoxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (tetrahydrofuran-3-ylcarbonyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- (4- {1- [ (propan-2-yloxy) acetyl ] piperidin-4-yl } butyl) -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (cyclopropylacetyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide;
n- {4- [1- (4, 4, 4-trifluorobutanoyl) piperidin-4-yl ] butyl } -1, 3-dihydro-2H-pyrrolo [3, 4-c ] pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
15. Compositions for treating the following diseases: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, dementia of the vascular or AD type, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive-compulsive disorders and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for preventing graft failure, and cystic fibrosis, said composition comprising an excipient and a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.
16. Compositions for treating the following diseases: inflammatory and tissue repair disorders; including rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases, including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, including breast, prostate, lung, colon, cervical, ovarian, skin, CNS, bladder, pancreatic, leukemia, lymphoma or lymphogranulomatous diseases, cachexia, inflammation associated with infection and viral infection, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia, comprising an excipient and a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.
17. A method of treating a patient for: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders including depression, schizophrenia, obsessive compulsive disorder and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for preventing graft failure and cystic fibrosis, the method comprising: administering to the patient a therapeutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.
18. A method of treating a patient for: inflammatory and tissue repair disorders; including rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer including breast cancer, prostate cancer, lung cancer, colon cancer, cervical cancer, ovarian cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, leukemia, lymphoma or lymphogranulomatosis, cachexia, inflammation associated with infection and viral infection including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia, the method comprising: administering to the patient a therapeutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.
19. A method of treating a patient for: hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm following subarachnoid hemorrhage, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunction, female sexual dysfunction, overactive bladder syndrome, spinal cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, alzheimer's disease, pain, multiple brain sclerosis, amyotrophic lateral sclerosis, huntington's disease, parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, premature labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders including depression, schizophrenia, obsessive compulsive disorder and bipolar disorders, epilepsy and seizure disorders, for reducing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for preventing graft failure and cystic fibrosis, the method comprising: administering to a patient a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof; and a therapeutically effective amount of one or more other therapeutic agents.
20. A method of treating a patient for: inflammatory and tissue repair disorders including rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; skin diseases including psoriasis, atopic dermatitis and ultraviolet-induced skin damage; autoimmune diseases including systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancers including breast, prostate, lung, colon, cervical, ovarian, skin, CNS, bladder, pancreatic, leukemia, lymphoma or lymphogranulomatous diseases, cachexia, inflammation associated with infection and certain viral infections including acquired immunodeficiency syndrome (AIDS), adult respiratory distress syndrome and ataxia telangiectasia or spleen cancer, comprising: administering to a patient a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof; and a therapeutically effective amount of one or more other therapeutic agents.
HK14102695.8A 2010-11-15 2011-11-11 Nampt and rock inhibitors HK1189589A (en)

Applications Claiming Priority (3)

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US61/413,722 2010-11-15
US61/474,015 2011-04-11
US61/525,405 2011-08-19

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HK1189589A true HK1189589A (en) 2014-06-13

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